Category: 96829-58-2

Forryan, James; Mishra, Vinita; Gibbons, Emily published the artcile< When the Cause Is Not Crystal Clear.>, Related Products of 96829-58-2, the main research area is .

There is no abstract available for this document.

The New England journal of medicine published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Related Products of 96829-58-2.

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

Karimabad, Mojgan Noroozi; Roostaei, Farzad; Mahmoodi, Mehdi; Hajizadeh, Mohammad Reza published the artcile< Evaluation of the effect of orlistatorlistat on expression of OCT4, Nanog, SOX2, and KLF4 genes in colorectal cancer SW40 cell line>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is orlistatorlistat OCT Nanog SOX KLF gene expression colorectal cancer; Colorectal Cance; Gene expression; Orlistat.

Orlistat drug is one of the most criticalanti-obesity drugs that widely used around the world. The aim of this study was evaluation the effect of orlistat on the expression of OCT4, Nanog, SOX2, and KLF4 genes in the colorectal cancer SW40 cell line. SW40 cell line was cultured in DMEM medium contained orlistat for 24h, and cell viability was assessed by MTT assay. The fold changes of expression of OCT4, NANOG, KLF4, and SOX2 at mRNA level against β-actin were determined by real-timePCR. Two-sample t-test and one-way ANOVA were used to compare the mean of expression of different genes in different groups and different concentrations; a significant level of 0.05 was considered in all tests. Our results showed a significant difference in cell viability, when different doses of Orlistat were used for 24 h. concentrations of 25 and 100μM reduce significantly the expression of OCT4 (P<0.05) and SOX2 (P<0.05) in the treated group in comparison to control (P<0.05). Also, the mRNA expression of KLF4 and Nanog was reduced significantly after treatment of SW40 cell lines was performed with 100μM doses of Orlistat (P<0.05). It appears that after further studies in animal and human phases, orlistat can be used for the treatment of Colorectal Cancer. Asian Pacific Journal of Cancer Prevention published new progress about Cell viability. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Ardissino, Maddalena; Vincent, Matthew; Hines, Oliver; Amin, Ravi; Eichhorn, Christian; Tang, Alice R; Collins, Peter; Moussa, Osama; Purkayastha, Sanjay published the artcile< Long-term cardiovascular outcomes after orlistat therapy in patients with obesity: a nationwide, propensity-score matched cohort study.>, SDS of cas: 96829-58-2, the main research area is Cardiovascular; Obesity; Orlistat; Weight loss; outcomes.

AIMS: The rising prevalence of obesity and its associated comorbidities represent a growing public health issue; in particular, obesity is known to be a major risk factor for cardiovascular disease. Despite the evidence behind the efficacy of orlistat in achieving weight loss in patients with obesity, no study thus far has quantified its long-term effect on cardiovascular outcomes. The purpose of this study is to explore long-term cardiovascular outcomes after orlistat therapy. METHODS AND RESULTS: A propensity-score matched cohort study was conducted on the nation-wide electronic primary and integrated secondary healthcare records of the Clinical Practice Research Datalink (CPRD). The 36 876 patients with obesity in the CPRD database who had completed a course of orlistat during follow-up were matched on a 1:1 basis with equal numbers of controls who had not taken orlistat. Patients were followed up for a median of 6 years for the occurrence of the primary composite endpoint of major adverse cardiovascular events (fatal or non-fatal myocardial infarction or ischaemic stroke), and a number of secondary endpoints including primary endpoint components individually, the occurrence of new-onset heart failure, coronary revascularization, new chronic kidney disease stage III+ (CKD3+), and all-cause mortality. During the median study follow-up of 6 years, the occurrence of major adverse cardiovascular events was lower in the orlistat cohort [hazard ratio (HR) 0.74; 95% confidence interval (CI) 0.66-0.83, P < 0.001]. Patients who took orlistat experienced lower rates of myocardial infarction (HR 0.77; 95% CI 0.66-0.88, P < 0.001) and ischaemic stroke (HR 0.68; 95% CI 0.56 to -0.84, P < 0.001) as well as new-onset heart failure (HR 0.79; 95% CI 0.67-0.94, P = 0.007). There was no differences in revascularization rates (HR 1.12; 95% CI 0.91-1.38, P = 0.27), but a lower rate of both CKD3+ development (HR 0.78; 95% CI 0.73-0.83, P < 0.001) and mortality (HR 0.39, 95% CI 0.36 to -0.41, P < 0.001) was observed. CONCLUSION: In this nation-wide, propensity-score matched study, orlistat was associated with lower rates of overall major adverse cardiovascular events, new-onset heart failure, renal failure, and mortality. This study adds to current evidence on the known improvements in cardiovascular risk factor profiles of orlistat treatment by suggesting a potential role in primary prevention. European heart journal. Cardiovascular pharmacotherapy published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

Cioccoloni, Giorgia; Aquino, Angelo; Notarnicola, Maria; Caruso, Maria Gabriella; Bonmassar, Enzo; Zonfrillo, Manuela; Caporali, Simona; Faraoni, Isabella; Villiva, Cristina; Fuggetta, Maria Pia; Franzese, Ornella published the artcile< Fatty acid synthase inhibitor orlistat impairs cell growth and down-regulates PD-L1 expression of a human T-cell leukemia line>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is orlistat fatty acid synthase programmed death ligand expression leukemia; FASN; PD-L1; leukemia.

Fatty Acid Synthase (FASN) is responsible for the de novo synthesis of fatty acids, which are involved in the preservation of biol. membrane structure, energy storage and assembly of factors involved in signal transduction. FASN plays a critical role in supporting tumor cell growth, thus representing a potential target for anti-cancer therapies. Moreover, this enzyme has been recently associated with increased PD-L1 expression, suggesting a role for fatty acids in the impairment of the immune response in the tumor microenvironment. Orlistat, a tetrahydrolipstatin used for the treatment of obesity, has been reported to reduce FASN activity, while inducing a sensible reduction of the growth potential in different cancer models. We have analyzed the effect of orlistat on different features involved in the tumor cell biol. of the T-ALL Jurkat cell line. In particular, we have observed that orlistat inhibits Jurkat cell growth and induces a perturbation of cell cycle along with a decline of FASN activity and protein levels. Moreover, the drug produces a remarkable impairment of PD-L1 expression. These findings suggest that orlistat interferes with different mechanisms involved in the control of tumor cell growth and can potentially contribute to decrease the tumor-associated immune-pathogenesis.

Journal of Chemotherapy (Abingdon, United Kingdom) published new progress about Antitumor agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Kim, Seongkyu; Kim, Je-Hein; Seok, Su Hyun; Park, Eun-Seok published the artcile< Anti-obesity effect with reduced adverse effect of the co-administration of mini-tablets containing orlistat and mini-tablets containing xanthan gum: In vitro and in vivo evaluation>, HPLC of Formula: 96829-58-2, the main research area is formulation tablet orlistat xanthan gum obesity; Anti-obesity; Oily leakage; Oily stool; Orlistat; Reduced adverse effect; Xanthan gum.

The purpose of this study was to develop an oral dosage form of orlistat for the treatment of obesity with reduced adverse effects, for example, fatty and oily stool that have been reported to be associated with the mechanism of action of orlistat. Based on the in vitro results obtained in this study, xanthan gum was selected as an oil-entrapping agent. Thus, the co-administration of mini-tablets containing orlistat and mini-tablets containing xanthan gum was proposed as the optimized dosage form for orlistat. The prepared mini-tablets showed an equivalent drug release profile with a similarity factor value, f2, more than 50 to that of com. marketed orlistat immediate-release capsules, Xenical capsules. In addition, the optimized formulation also showed the in vivo anti-obesity effects similar to those of Xenical capsules. In particular, the anal. of feces excreted by Sprague-Dawley rats revealed that the optimized formulation resulted in significantly less oily stool, steatorrhea, than Xenical capsules (P < 0.05). Consequently, the proposed formulation, the co-administration of mini-tablets containing orlistat and mini-tablets containing xanthan gum, may be considered as a promising anti-obesity treatment with reduced adverse effects related to orlistat. International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, HPLC of Formula: 96829-58-2.

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

Šrámková, Petra; Fried, Martin published the artcile< Antiobesity drugs before and after bariatric surgery - how to make the best use of them.>, Formula: C29H53NO5, the main research area is bariatric surgery; liraglutide; multifunctional peptides; naltrexone-bupropion; obesity; preoperative weight reduction; set point; weight gain after bariatric surgery.

Obesity as a chronic, serious, and progressive lifelong disease requires an active approach to treatment. Treatment means necessary adjustment of lifestyle with suitable regular physical activity, including pharmacological or bariatric support. Current pharmacological treatment can be an effective helper in the preparation for the surgical treatment of obesity (bariatric and metabolic operations), and in greater adherence of the patient to the necessary regime changes in life and in preoperative weight reduction. With the lapse of time after surgical treatment, in many cases we indicate the start of pharmacological treatment if the weight increases again. We do not yet know the appropriate types of patients and the exact indications for specific therapeutic modalities – a suitable antiobesity drug or type of bariatric surgery. The best long-term results come from a combination of at least two of these options, along with a lifestyle change. Among modern antiobesity drugs, there are naltrexone-bupropion and liraglutide. Orlistat can be mentioned from older ones.

Casopis lekaru ceskych published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Formula: C29H53NO5.

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

Sridhar, S. N. C.; Palawat, Saksham; Paul, Atish T. published the artcile< Design, synthesis, biological evaluation and molecular modelling studies of indole glyoxylamides as a new class of potential pancreatic lipase inhibitors>, Synthetic Route of 96829-58-2, the main research area is indole glyoxylamides pancreas lipase inhibition mol dynamics antiobesity; Indole glyoxylamides; Inhibition kinetics; Molecular dynamics; Orlistat; Pancreatic lipase.

A series of eighteen indole glyoxylamide analogs were synthesized, characterized and evaluated for their pancreatic lipase inhibitory activity. Porcine pancreatic lipase (Type II) was used with 4-nitrophenyl butyrate (as substrate) for the in vitro assay. Compound 8f exhibited competitive inhibition against pancreatic lipase with IC50 value of 4.92 μM, comparable to that of the standard drug, orlistat (IC50 = 0.99 μM). Compounds 7a-i and 8a-i were subjected to mol. docking into the active site of human PL (PDB ID: 1LPB) wherein compound 8f possessed a potential MolDock score of -153.037 kcal/mol. Mol. dynamics simulation of 8f complexed with pancreatic lipase, confirmed the role of aromatic substitution in stabilizing the ligand through hydrophobic interactions (maximum observed RMSD = 3.5 Å).

Bioorganic Chemistry published new progress about Amides Role: BSU (Biological Study, Unclassified), PRP (Properties), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation) (indole glyoxylamides). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Synthetic Route of 96829-58-2.

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

Cui, Xinyuan; Chen, Xiaojun; Li, Yifu; Fu, Xiao; Song, Pan’ai; Xiao, Li; Sun, Lin; Liu, Hong; Zhu, Xuejing; Yuan, Shuguang published the artcile< Oxalate crystal-related acute renal injury caused by orlistat: A case report.>, Category: amides-buliding-blocks, the main research area is acute oxalic acid nephropathy; hyperoxaluria; orlistat.

We reported a case of oxalate crystal-related acute kidney injury caused by orlistat. The patient was admitted for nephrotic syndrome and acute kidney injury. The pathomorphological assessment of renal biopsy showed intratubular oxalate crystals. The patient reported that she had taken orlistat regularly to loss weight for more than a year. This patient had a habit of drinking vegetable soup and strong herbal tea daily. Orlistat, an intestinal lipase inhibitor, may cause secondary hyperoxaluria, that is, intestinal hyperoxaluria. Dietary habits could be a common precipitating factor for orlistat-relevant hyperoxaluria. It was comprehensively considered to be oxalate crystal-related acute renal injury, and the patient’s renal function recovered gradually after drug withdrawal. Clinicians should pay attention to screening drug-related acute kidney injury including orlistat when observing patients with unexplained acute kidney injury, and renal biopsy should be performed if necessary. It is also important to warn people who take the orlistat for weight loss about the side effects of this drug so as to adjust the eating habits.

Zhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Category: amides-buliding-blocks.

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

Zhang, Zhanwen; Liu, Shaoyu; Ma, Hui; Nie, Dahong; Wen, Fuhua; Zhao, Jing; Sun, Aixia; Yuan, Gongjun; Su, Shu; Xiang, Xianhong; Hu, Ping; Tang, Ganghua published the artcile< Validation of R-2-[18F]Fluoropropionic Acid as a Potential Tracer for PET Imaging of Liver Cancer>, Application In Synthesis of 96829-58-2, the main research area is liver cancer radioactivity tracer PET imaging; 2-[18F]Fluoropropionic acid; Liver cancer; Positron emission tomography; R,S-enantiomer; Uptake mechanism.

2-[18F]Fluoropropionic acid (RS-[18F]FPA) has shown potential value as a short-chain fatty acid positron emission tomog. (PET) tracer for the detection of liver cancer. However, RS-[18F]FPA is a mixture of 2-R-[18F]fluoropropionic acid (R-[18F]FPA) and 2-S-[18F]fluoropropionic acid (S-[18F]FPA). The aim of this study is to validate the feasibility of R-[18F]FPA in preclin. PET imaging of liver cancer and to compare the use of R-[18F]FPA with that of RS-[18F]FPA and S-[18F]FPA. A comparative study of R-[18F]FPA, RS-[18F]FPA, S-[18F]FPA, and [18F]FDG micro-PET imaging was performed in HepG2 and SK-Hep-1 tumor-bearing mice. A comparison of R-[18F]FPA uptake with that of S-[18F]FPA by HepG2 and SK-Hep-1 cells was made at different time points. Addnl., in vivo blocking experiments in HepG2 and SK-Hep-1 tumor models were conducted with orlistat and 3-nitropropionic acid (3-NP). In vitro blocking experiments with orlistat or 3-NP were performed with HepG2 and SK-Hep-1 cells. The radioactivity uptake values of R-[18F]FPA were comparable to those of RS-[18F]FPA but were higher than those of S-[18F]FPA and 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) in HepG2 tumors. The radioactivity uptake values of R-[18F]FPA in large HepG2 tumors were lower than those of [18F]FDG (P < 0.05), while R-[18F]FPA PET was significantly superior to [18F]FDG PET in detecting small tumors (both SK-Hep-1 and HepG2 tumors). The in vivo PET imaging experiments showed that R-[18F]FPA uptake in HepG2 tumor-bearing mice was blocked by 19.3 % and 31.8 % after treatment with orlistat and 3-NP, resp. The radioactivity uptake values of R-[18F]FPA in SK-Hep-1 tumor-bearing mice was blocked by 39.5 % with orlistat. R-[18F]FPA seems to be more potential than S-[18F]FPA as an optically pure PET probe, with effective compensation for the deficiencies of [18F]FDG, particularly in PET imaging of small liver cancer. The uptake mechanism of [18F]FPA in liver cancer may be related to fatty acid synthesis and the tricarboxylic acid cycle. However, compared with the racemic RS-[18F]FPA, the possible advantages of R-enantiomer R-[18F]FPA still needs further research. Molecular Imaging and Biology published new progress about Adenocarcinoma. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

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

Dully, Michele; Brasnett, Christopher; Djeghader, Ahmed; Seddon, Annela; Neilan, John; Murray, David; Butler, James; Soulimane, Tewfik; Hudson, Sarah P. published the artcile< Modulating the release of pharmaceuticals from lipid cubic phases using a lipase inhibitor>, Related Products of 96829-58-2, the main research area is pharmaceutical lipid cubic system controlled release monoglyceride lipase inhibitor; Controlled delivery; Enzyme degradation; Hydrophobic active pharmaceuticals; Lipase inhibitor; Lipid cubic phase; SAXS.

Lipid cubic phase formulations have gained recognition as potential controlled delivery systems for a range of active pharmaceutical and biol. agents on account of their desirable physiochem. properties and ability to encapsulate both hydrophobic and hydrophilic mols. The most widely studied lipid cubic systems are those of the monoacylglycerol lipid family. These formulations are susceptible to lipolysis by a variety of enzymes, including lipases and esterases, which attack the ester bond present on the lipid chain bridging the oleic acid component to the glycerol backbone. The release of poorly soluble mols. residing in the lipid membrane portions of the phase is limited by the breakdown of the matrix; thus, presenting a potential means for further controlling and sustaining the release of therapeutic agents by targeting the matrix stability and its rate of degradation The aims of the present study were twofold: to evaluate an approach to regulate the rate of degradation of lipid cubic phase drug delivery systems by targeting the enzyme interactions responsible for their demise; and to study the subsequent drug release profiles from bulk lipid cubic gels using model drugs of contrasting hydrophobicity. Here, hybrid materials consisting of cubic phases with monoacylglycerol lipids of different chain lengths formulated with a potent lipase inhibitor tetrahydrolipstatin were designed. Modulation of the release of a hydrophobic model pharmaceutical, a clofazimine salt, was obtained by exploiting the matrixes’ enzyme-driven digestion. A stable cubic phase is described, displaying controlled degradation with at least a 4-fold improvement compared to the blank systems shown in inhibitor-containing cubic systems. Sustained release of the model hydrophobic pharmaceutical was studied over 30 days to highlight the advantage of incorporating an inhibitor into the cubic network to achieve tunable lipid release systems. This is done without neg. affecting the structure of the matrix itself, as shown by comprehensive small-angle x-ray scattering experiments

Journal of Colloid and Interface Science published new progress about Biodegradation kinetics. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Related Products of 96829-58-2.

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