Tag: 400-500

Distribution of methotrexate in rat tissues was written by Newbold, P. C. H.. And the article was included in British Journal of Dermatology in 1974.Quality Control of Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate This article mentions the following:

Following i.p. injection of tritiated methotrexate di-Na salt (I di-Na salt) [7413-34-5], the amounts of I taken up by the skin and liver of rats were doubled by exptl. folic acid [59-30-3] depletion. In contrast, folate deficiency did not significantly increase I uptake by the kidneys or intestines. Skin uptake of I was increased about 6-fold by prior stripping (psoriasis model); hepatic uptake was still marked in this model. I taken up by the tissues was partially displaced by pteridines with an infinity for dehydrofolate reductase. Displacement was most efficient with I itself, but also significant with both dihydrofolate [4033-27-6] and folic acid and measurable with leucovorin [58-05-9]; 5-methyl folate [53464-60-1] had virtually no effect. Thus, a risk of hepatic injury is probably inseparable from the therapeutic action of I in psoriasis. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Quality Control of Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Quality Control of Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Selective Cell Penetrating Peptide-Functionalized Polymersomes Mediate Efficient and Targeted Delivery of Methotrexate Disodium to Human Lung Cancer In Vivo was written by Yang, Weijing;Xia, Yifeng;Fang, Yuan;Meng, Fenghua;Zhang, Jian;Cheng, Ru;Deng, Chao;Zhong, Zhiyuan. And the article was included in Advanced Healthcare Materials in 2018.Application of 7413-34-5 This article mentions the following:

It is a long challenge to develop nanomedicines that simultaneously possess tumor cell selectivity and penetration functions. Here, it is reported that selective cell penetrating peptide (RLWMRWYSPRTRAYGC)-functionalized polymersomes (SCPP-PS) mediate efficient and targeted delivery of methotrexate disodium (MTX) to human lung cancer in vivo. SCPP-PS with an SCPP d. of 18.7% is self-crosslinked, has a small size (63-65 nm), and high MTX loading (up to 19.4 wt%), shows selective uptake and fast penetration into A549 lung cancer cells, and efficiently releases MTX intracellularly. Interestingly, MTX-loaded SCPP-PS (MTX-SCPP-PS) displays much lower IC₅₀ than those of MTX-PS and free MTX. Installing SCPP to polymersomes has no detrimental effect to their long blood circulation time but significantly increases drug accumulation in A549 tumor (5.3% injected dose per g at 8 h post injection). Remarkably, SCPP-PS exhibits deep penetration in to A549 tumors. MTX-SCPP-PS completely inhibits tumor progression and significantly improves survival rates in mice bearing A549 lung tumor xenografts as compared to MTX-PS and free MTX groups (median survival time: 75 vs 45 and 38 d, resp.), without causing noticeable adverse effects. These results highlight that functionalization of nanomedicines with SCPP is a feasible strategy to achieve efficient and targeted tumor therapy. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Application of 7413-34-5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Application of 7413-34-5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

High-throughput screening of 756 chemical contaminants in aquaculture products using liquid chromatography/quadrupole time-of-flight mass spectrometry was written by Bai, Mingkai;Tang, Ruixue;Li, Guorong;She, Wenhai;Chen, Gangjun;Shen, Hongmei;Zhu, Suqin;Zhang, Hongwei;Wu, Haohao. And the article was included in Food Chemistry: X in 2022.Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

A high-throughput screening method embracing 756 multiclass chem. contaminants in aquaculture products was developed using modified QuEChERS extraction coupled with liquid chromatog./quadrupole time-of-flight mass spectrometry. A mega-database with retention time/accurate mass data for 524 pesticides, 182 veterinary drugs, 32 persistent organic pollutants and 18 marine toxins was established for compound identification via retrospective library searching. In the four representative matrixes (muscle tissues of tilapia and grouper, and edible portions of oyster and scallop), all the database compounds showed acceptable recovery and repeatability with the screening detection limit and limit of quantification below 0.01 mg/kg for >90% of them. The matrix-matched calibration revealed acceptable quant. property of the method in terms of linear range, linearity, and matrix effect, and fish muscle samples showed stronger matrix effect than shellfish samples. Anal. of 64 real-life samples from aquaculture farms and retail markets evidenced applicability of the proposed method to high-throughput screening scenarios. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Exposure to high-altitude environment is associated with drug transporters change: microRNA-873-5p-mediated alteration of function and expression levels of drug transporters under hypoxia was written by Duan, Yabin;Bai, Xue;Yang, Jianxin;Zhou, Yang;Gu, Wenqi;Liu, Guiqin;Wang, Qian;Zhu, Junbo;La, Linli;Li, Xiangyang. And the article was included in Drug Metabolism & Disposition in 2022.Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Hypoxia is the main characteristic of a high-altitude environment, affecting drug metabolism However, so far, the mechanism of miRNA involved in the regulation of drug metabolism and transporters under high-altitude hypoxia is still unclear. This study aims to investigate the functions and expression levels of multidrug resistance protein 1 (MDR1), multidrug resistance-associated protein 2 (MRP2), breast cancer resistance protein (BCRP), peptide transport 1 (PEPT1), and organic anion-transporting polypeptides 2B1 (OATP2B1) in rats and Caco-2 cells after exposure to high-altitude hypoxia. The protein and mRNA expression of MDR1, MRP2, BCRP, PEPT1, and OATP2B1 were determined by Western blot and qPCR. The functions of MDR1, MRP2, BCRP, PEPT1, and OATP2B1 were evaluated by determining the effective intestinal permeability and absorption rate constants of their specific substrates in rats under high-altitude hypoxia, and uptake and transport studies were performed on Caco-2 cells. To screen the miRNA associated with hypoxia, Caco-2 cells were examined by high throughput sequencing. We observed that the miR-873-5p was significantly decreased under hypoxia and might target MDR1 and pregnane X receptor (PXR). To clarify whether miR-873-5p regulates MDR1 and pregnane X receptor (PXR) under hypoxia, Caco-2 cells were transfected with mimics or inhibitors of miR-873-5p and neg. control (NC). The function and expression of drug transporters were found to be significantly increased in rats and Caco-2 cells under hypoxia. We found that miR-873-5p regulated MDR1 and PXR expression. Herein, it is shown that miRNA may affect the expression of drug transporter and nuclear receptor under hypoxia. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Small conductance calcium-activated potassium channels and nitric oxide/cGMP pathway mediate cardioprotective effects of Croton urucurana Baill. In hypertensive rats was written by Lopes, Katiana Simoes;Marques, Aline Aparecida Macedo;Moreno, Karyne Garcia Tafarelo;Lorencone, Bethania Rosa;Leite, Patricia Regina Terco;da Silva, Gabriela Pereira;dos Santos, Ariany Carvalho;Souza, Roosevelt Isaias Carvalho;Gasparotto, Francielly Mourao;Cassemiro, Nadla Soares;Lourenco, Emerson Luiz Botelho;Klider, Lislaine Maria;Manfron, Jane;Silva, Denise Brentan;Gasparotto, Arquimedes Junior. And the article was included in Journal of Ethnopharmacology in 2022.Reference of 10238-21-8 This article mentions the following:

(Euphorbiaceae), popularly known as sangue de draga is a Brazilian species widely used in traditional medicine for cardiovascular ailments. To investigate the cardiovascular effects of the C. urucurana extract in spontaneously hypertensive rats (SHRs).Leaves from C. urucurana were collected and morphoanatomically characterized. The ethanol-soluble fraction (ESCU) was obtained and analyzed by LC-DAD-MS. Using female Wistar rats we investigated the acute toxicity of ESCU. Then, SHRs (six months old) received vehicle, hydrochlorothiazide (25 mg/kg), or ESCU (30, 100, 300 mg/kg) for 28 days. At the beginning and at the end of treatments, urine samples were obtained to assess renal function. At the end of the trial period, the blood pressure, mesenteric vascular beds (MVBs) reactivity, and electrocardiog. profile were evaluated. Serum angiotensin-converting enzyme activity, as well as urea, creatinine, sodium, potassium, nitrite, malondialdehyde, nitrotyrosine, and aldosterone levels were determined Relative organ weights and histopathol. anal. were performed. Finally, the cardiac function on a Langendorff system, as well as the mol. mechanisms involved in the vasodilator effects of ESCU in MVBs were also investigated. The compounds annotated from ESCU by LC-DAD-MS included mainly phenylpropanoid derivatives, alkaloids, O-glycosylated megastigmanes, glycosylated flavonoids, flavan-3-ols, and others, such as quercetin O-deoxyhexosyl-hexoside, magnoflorine, reticuline, and taspine. None of the animals showed any signs of toxicity. Male SHRs treated only with the vehicle showed important cardiovascular changes, including a reduction in renal function, increase in serum oxidative stress, and hemodynamic, electrocardiog., and morphol. changes typical of hypertensive disease. Moreover, parameters of cardiac function, including left ventricular developed pressure, peak rate of contraction, peak rate of relaxation, and the rate pressure product were significantly altered, showing a significant impairment of ventricular function. All ESCU-doses presented a significant cardioprotective effect in SHRs rats. The 28-day treatment normalized the hemodynamic, electrocardiog., morphol., and renal impairments, as well as reversed the changes in ventricular function induced by hypertension. In MVBs with an intact endothelium, ESCU (0.1, 0.3, and 1 mg) dose-dependently induced vasodilation. Endothelium removal or the inhibition of nitric oxide synthase prevented the vasodilatory effect of ESCU. Perfusion with a physiol. saline solution that contained KCl, tetraethylammonium, or apamin also abolished the vasodilatory effect of ESCU. Prolonged ESCU-treatment showed significant cardioprotective effects in SHRs. Moreover, the data showed the role of nitric oxide and calcium-activated small conductance potassium channels in the cardiovascular effects of ESCU. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Reference of 10238-21-8).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Reference of 10238-21-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The effect of Glibenclamide on somatosensory evoked potentials after cardiac arrest in rats was written by Lachance, Brittany Bolduc;Wang, Zhuoran;Badjatia, Neeraj;Jia, Xiaofeng. And the article was included in Neurocritical Care in 2022.Category: amides-buliding-blocks This article mentions the following:

Abstract: Background: Science continues to search for a neuroprotective drug therapy to improve outcomes after cardiac arrest (CA). The use of glibenclamide (GBC) has shown promise in preclin. studies, but its effects on neuroprognostication tools are not well understood. We aimed to investigate the effect of GBC on somatosensory evoked potential (SSEP) waveform recovery post CA and how this relates to the early prediction of functional outcome, with close attention to arousal and somatosensory recovery, in a rodent model of CA. Methods: Sixteen male Wistar rats were subjected to 8-min asphyxia CA and assigned to GBC treatment (n = 8) or control (n = 8) groups. GBC was administered as a loading dose of 10 μg/kg i.p. 10 min after the return of spontaneous circulation, followed by a maintenance dosage of 1.6 μg/kg every 8 h for 24 h. SSEPs were recorded from baseline until 150 min following CA. Coma recovery, arousal, and brainstem function, measured by subsets of the neurol. deficit score (NDS), were compared between both groups. SSEP N10 amplitudes were compared between the two groups at 30, 60, 90, and 120 min post CA. Results: Rats treated with GBC had higher sub-NDS scores post CA, with improved arousal and brainstem function recovery (P = 0.007). Both groups showed a gradual improvement of SSEP N10 amplitude over time, from 30 to 120 min post CA. Rats treated with GBC showed significantly better SSEP recovery at every time point (P < 0.001 for 30, 60, and 90 min; P = 0.003 for 120 min). In the GBC group, the N10 amplitude recovered to baseline by 120 min post CA. Quantified Cresyl violet staining revealed a significantly greater percentage of damage in the control group compared with the GBC treatment group (P = 0.004). Conclusions: Glibenclamide improves coma recovery, arousal, and brainstem function after CA with decreased number of ischemic neurons in a rat model. GBC improves SSEP recovery post CA, with N10 amplitude reaching the baseline value by 120 min, suggesting early electrophysiol. recovery with this treatment. This medication warrants further exploration as a potential drug therapy to improve functional outcomes in patients after CA. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Category: amides-buliding-blocks).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Enhancement of the brain delivery of methotrexate with administration of mid-chain ester prodrugs: In vitro and in vivo studies was written by Fattahi, Nadia;Ramazani, Ali;Hamidi, Mehrdad;Parsa, Maliheh;Rostamizadeh, Kobra;Rashidzadeh, Hamid. And the article was included in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 2021.Synthetic Route of C20H20N8Na2O5 This article mentions the following:

In the present study, with the aim of improving the permeability of methotrexate (MTX) to the brain, the lipophilic MTX prodrugs containing the ester functional moiety were synthesized. The chem. structure of synthesized prodrugs was characterized and confirmed by FT-IR, NMR and mass spectral studies. Based on the results of in vitro cytotoxic studies, all of the synthesized prodrugs led to decrease in the IC50 in 72 h on U87 cancer cell line and the best result was observed for dihexyl methotrexate (MTX-DH) in comparison with free MTX, which led to decrease the IC50 amount up to 6 folds. In addition, in vivo toxicity on Artemia salina (A. salina) showed that the lipophilic MTX prodrugs have been able to partially mask the toxic profile of free MTX, at the same concentrations These findings were also in compliance with hemolysis assay results, which confirm that the conjugates has not made the drug more toxic. Furthermore, in vivo study in rat model, was employed to determine the simultaneous drug concentration in brain and plasma. According to the obtained results, the brain-to-plasma concentration ratios (Kp values) of MTX-DH and dioctyl methotrexate (MTX-DO) groups were significantly higher compared with free MTX. Moreover, the uptake clearance of MTX by brain parenchyma increased significantly (3.85 and 9.08-time increased for MTX-DH and MTX-DO prodrugs, resp.). These findings indicate that the synthesized lipophilic MTX prodrugs are non-toxic and able to enhance brain penetration of MTX. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Synthetic Route of C20H20N8Na2O5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Synthetic Route of C20H20N8Na2O5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Bioaccumulation and bioamplification of pharmaceuticals and endocrine disruptors in aquatic insects was written by Veseli, Marina;Rozman, Marko;Vilenica, Marina;Petrovic, Mira;Previsic, Ana. And the article was included in Science of the Total Environment in 2022.Category: amides-buliding-blocks This article mentions the following:

Environmental fate of emerging contaminants such as pharmaceuticals and endocrine disrupting compounds at the aquatic terrestrial boundary are largely unexplored. Aquatic insects connect aquatic and terrestrial food webs as their life cycle includes aquatic and terrestrial life stages, thus they represent an important inter-habitat linkage not only for energy and nutrient flow, but also for contaminant transfer to terrestrial environments. We measured the concentrations of pharmaceuticals and endocrine disrupting compounds in the larval and adult tissues (last larval stages and teneral adults) of five Odonata species sampled in a wastewater-impacted river, in order to examine their bioaccumulation and bioamplification at different taxonomic levels. Twenty different compounds were bioaccumulated in insect tissues, with majority having higher concentrations (up to 90% higher) in aquatic larvae compared to terrestrial adults (reaching 88 ng/g for 1H-benzotriazole). However, increased concentration in adults was observed for seven compounds in at least one suborder (41% of the accumulated), confirming contaminants bioamplification across the metamorphosis. Both, bioaccumulation and bioamplification differed at various taxa levels; the order (Odonata), suborder (Anisoptera and Zygoptera) and species level. Highest variability was observed between Anisoptera and Zygoptera, due to the underlying differences in their ecol. Generally, Zygoptera had higher concentrations of contaminants in both larvae and adults. Addnl., we aimed at predicting effects of contaminant properties on bioaccumulation and bioamplification patterns using the commonly used physicochem. and pharmacokinetic descriptors on both order and suborder levels, however, neither of the two processes could be consistently predicted with simple linear models. Our study highlights the importance of taxonomy in studies aiming at advancing the understanding of contaminant exchange between aquatic and terrestrial food webs, as higher taxonomic categories include ecol. diverse groups, whose contribution to “the dark side of subsidies” could substantially differ. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Category: amides-buliding-blocks).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Experimental and modeling investigation of Glibenclamide solubility in supercritical carbon dioxide was written by Esfandiari, Nadia;Sajadian, Seyed Ali. And the article was included in Fluid Phase Equilibria in 2022.Product Details of 10238-21-8 This article mentions the following:

Optimized production of micro and nanoparticles using the supercritical fluid technique requires information on the solubility of pharmaceutical materials in the supercritical fluid. In this article, Glibenclamide solubility in the SC-CO₂ was investigated for the first time at the temperature range 0f 308-338 K and pressure range of 12-30 MPa. Under this condition, the mole fraction of Glibenclamide was determined in the range 0.8 x 10^-6 to 8.03 x 10^-5. Furthermore, the six empirical models (i.e. Chrastil, Bartle et al., Mendez-Santiago and Teja (MST), Sparks et al., Bian et al., Sodeifian et al.) and PR-EoS with vdW2 mixing rule were utilized to correlate the solubility The results confirmed that Sodeifian et al. and MST models exhibited the highest accuracy with resp. R_adj of 0.996 and 0.9859. Finally, the total (41.65 kJ mol^-1), vaporization (65.5 kJ mol^-1), and solvation. (-23.85 kJ mol^-1) enthalpies were estimated by Chrastil’s model and Bartle et al. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Product Details of 10238-21-8).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Product Details of 10238-21-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Pharmacological and therapeutic properties of carrier bound methotrexate against tumor confined to a third space body compartment was written by Chu, Barbara C. F.;Howell, Stephen B.. And the article was included in Journal of Pharmacology and Experimental Therapeutics in 1981.Recommanded Product: 7413-34-5 This article mentions the following:

The pharmacokinetics and therapeutic effectiveness of Na methotrexate (MTX)(I Na salt) [7413-34-5] and MTX covalently bound to bovine serum albumin (MTX-BSA) and poly-l-lysine, MW 3,000 (MTX-PLL 3K) or MW 40,000 to 60,000 (MTX-PLL 40-60K) were compared when these drugs were injected directly into the pleural cavities of BDF, mice containing the L1210 tumor. Simultaneous measurements of drug levels in both pleural fluid and blood after a single dose demonstrated that free MTX and MTX-PLL 3K were cleared from the pleural cavity and blood within 4 h, MTX-PLL 40K-60K was cleared within 2 h, and MTX-BSA was still present in the tumor compartment at 48 h. The coupling of MTX to these carriers increased its toxicity by extending the half-life of MTX-BSA within the animal and by incorporating a toxic PLL derivative as a carrier. At equitoxic doses, a single dose of MTX-BSA gave a peak increase in lifespan (ILS) of 50% (at 35 mg/kg) compared with a peak ILS of 30 to 35% for both free drug (at 95 mg/kg) and the MTX-PLL derivatives (at 1.4-6 mg/kg). Systemic administration of sufficient Ca leucovorin [1492-18-8] to provide partial marrow protection compromised the antitumor activity of both MTX and MTX-BSA in the pleural cavity, and although leucovorin permitted higher doses to be used, this resulted in only a small increase in peak ILS for MTX-BSA on a single dose schedule. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Recommanded Product: 7413-34-5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Recommanded Product: 7413-34-5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics