Category: 53902-12-8

Enhanced nose-to-brain delivery of tranilast using liquid crystal formulations was written by See, Gerard Lee;Arce, Florencio Jr.;Dahlizar, Sabrina;Okada, Akie;Bin Mohd. Fadli, Muhammad Fikri;Hijikuro, Ichiro;Itakura, Shoko;Katakura, Masanori;Todo, Hiroaki;Sugibayashi, Kenji. And the article was included in Journal of Controlled Release in 2020.Application of 53902-12-8 This article mentions the following:

Intranasal administration is poised as a competent method in delivering drugs to the brain, because the nasal route has a direct link with the central nervous system bypassing the formidable blood-brain barrier. C₁₇-monoglycerol ester (MGE) and glyceryl monooleate (GMO) as liquid crystal (LC)-forming lipids possess desirable formulation characteristics as drug carriers for intranasally administered drugs. This study investigated the effect of LC formulations on the pharmacokinetics of tranilast (TL), a lipophilic model drug, and its distribution in the therapeutic target regions of the brain in rats. The anatomical biodistribution of LC formulations was monitored using micro-computed tomog. tandem in vivo imaging systems. MGE and GMO effectively formed LC with suitable particle size, zeta potential, and viscosity supporting the delivery of TL to the brain. MGE and GMO LC formulations enhanced brain uptake by 10- to 12-fold and 2- to 2.4- fold, resp., compared with TL solution The olfactory bulb had the highest TL concentration and fluorescent signals among all the brain regions, indicating a direct nose-to-brain delivery pathway of LC formulations. LC-forming lipids, MGE and GMO, are potential biomaterials in formulations intended for intranasal administration. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Application of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Application of 53902-12-8

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

Tranilast as an Adjunctive Therapy in Hospitalized Patients with Severe COVID- 19: A Randomized Controlled Trial was written by Saeedi-Boroujeni, Ali;Nashibi, Roohangiz;Ghadiri, Ata A.;Nakajima, Motowo;Salmanzadeh, Shokrollah;Mahmoudian-Sani, Mohammad-Reza;Hanafi, Mohammad Ghasem;Sharhani, Asaad;Khodadadi, Ali. And the article was included in Archives of Medical Research in 2022.Quality Control of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

Tranilast is a potential NLRP3 inflammasome inhibitor that may relieve progressive inflammation due to COVID-19. To evaluate the therapeutic effects of Tranilast in combination with antiviral drugs in non-ICU-admitted hospitalized patients with COVID-19. This study was an open-label clin. trial that included 72 hospitals admitted patients with severe COVID-19 at Razi Hospital, Ahvaz, Iran, from July 2020-August 2020. These patients were randomly assigned in a 1:1 ratio to control (30) and intervention groups (30). Patients in the control group received antiviral therapy, while patients in the intervention group received Tranilast (300 mg daily) in addition to the antiviral drugs for Seven days. The collected data, including the expression of inflammatory cytokine, laboratory tests, and clin. findings, was used for intragroup comparisons. The intervention group showed significantly lower levels of NLR (p = 0.001), q-CRP (p = 0.002), IL-1 (p = 0.001), TNF (p = 0.001), and LDH (p = 0.046) in comparison with the control group. The effect of intervention was significant in increasing the o2 saturation (F = 7.72, p = 0.007). Long hospitalization (four days or above) was 36.6% in the Tranilast and 66.6% in the control group (RR = 0.58; 95% CI: 0.38-1.06, p = 0.045). In the Tranilst and control groups, one and four deaths or hospitalization in ICU were observed resp. (RR = 0.31; 95% CI: 0.03-2.88, p = 0.20). Tranilast might be used as an effective and safe adjuvant therapy and enhance the antiviral therapy′s efficacy for managing patients with COVID-19. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Quality Control of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. 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.Quality Control of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

Neuroprotective Effects of Cannabidiol but Not Δ9-Tetrahydrocannabinol in Rat Hippocampal Slices Exposed to Oxygen-Glucose Deprivation: Studies with Cannabis Extracts and Selected Cannabinoids was written by Landucci, Elisa;Mazzantini, Costanza;Lana, Daniele;Davolio, Pier Luigi;Giovannini, Maria Grazia;Pellegrini-Giampietro, Domenico E.. And the article was included in International Journal of Molecular Sciences in 2021.SDS of cas: 53902-12-8 This article mentions the following:

Over the past 10 years, a number of scientific studies have demonstrated the therapeutic potential of cannabinoid compounds present in the Cannabis Sativa and Indica plants. However, their role in mechanisms leading to neurodegeneration following cerebral ischemia is yet unclear. We investigated the effects of Cannabis extracts (Bedrocan, FM2) or selected cannabinoids (Δ9-tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabigerol) in rat organotypic hippocampal slices exposed to oxygen-glucose deprivation (OGD), an in vitro model of forebrain global ischemia. Cell death in the CA1 subregion of slices was quantified by propidium iodide fluorescence, and morphol. anal. and tissue organization were examined by immunohistochem. and confocal microscopy. Incubation with the Bedrocan extract or THC exacerbated, whereas incubation with the FM2 extract or cannabidiol attenuated CA1 injury induced by OGD. Δ9-THC toxicity was prevented by CB1 receptor antagonists, the neuroprotective effect of cannabidiol was blocked by TRPV2, 5-HT1A, and PPARγ antagonists. Confocal microscopy confirmed that CBD, but not THC, had a significant protective effect toward neuronal damage and tissue disorganization caused by OGD in organotypic hippocampal slices. Our results suggest that cannabinoids play different roles in the mechanisms of post-ischemic neuronal death. In particular, appropriate concentrations of CBD or CBD/THC ratios may represent a valid therapeutic intervention in the treatment of post-ischemic neuronal death. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8SDS of cas: 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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 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.SDS of cas: 53902-12-8

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

Drug repurposing screening identifies tioconazole as an ATG4 inhibitor that suppresses autophagy and sensitizes cancer cells to chemotherapy was written by Liu, Pei-Feng;Tsai, Kun-Lin;Hsu, Chien-Jen;Tsai, Wei-Lun;Cheng, Jin-Shiung;Chang, Hsueh-Wei;Shiau, Chung-Wai;Goan, Yih-Gang;Tseng, Ho-Hsing;Wu, Chih-Hsuan;Reed, John C.;Yang, Lee-Wei;Shu, Chih-Wen. And the article was included in Theranostics in 2018.Application of 53902-12-8 This article mentions the following:

Tumor cells require proficient autophagy to meet high metabolic demands and resist chemotherapy, which suggests that reducing autophagic flux might be an attractive route for cancer therapy. However, this theory in clin. cancer research remains controversial due to the limited number of drugs that specifically inhibit autophagy-related (ATG) proteins. We screened FDA-approved drugs using a novel platform that integrates computational docking and simulations as well as biochem. and cellular reporter assays to identify potential drugs that inhibit autophagy-required cysteine proteases of the ATG4 family. The effects of ATG4 inhibitors on autophagy and tumor suppression were examined using cell culture and a tumor xenograft mouse model. Tioconazole was found to inhibit activities of ATG4A and ATG4B with an IC50 of 1.3μM and 1.8μM, resp. Further studies based on docking and mol. dynamics (MD) simulations supported that tioconazole can stably occupy the active site of ATG4 in its open form and transiently interact with the allosteric regulation site in LC3, which explained the exptl. observed obstruction of substrate binding and reduced autophagic flux in cells in the presence of tioconazole. Moreover, tioconazole diminished tumor cell viability and sensitized cancer cells to autophagy-inducing conditions, including starvation and treatment with chemotherapeutic agents. Tioconazole inhibited ATG4 and autophagy to enhance chemotherapeutic drug-induced cytotoxicity in cancer cell culture and tumor xenografts. These results suggest that the antifungal drug tioconazole might be repositioned as an anticancer drug or chemosensitizer. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Application of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Application of 53902-12-8

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

Screening and evaluation of potential inhibitors against vaccinia virus from 767 approved drugs was written by Wu, Jiajing;Liu, Qiang;Xie, Hui;Chen, Ruifeng;Huang, Weijin;Liang, Chunnan;Xiao, Xinyue;Yu, Yongxin;Wang, Youchun. And the article was included in Journal of Medical Virology in 2019.Related Products of 53902-12-8 This article mentions the following:

The development of therapies for human smallpox is needed due to the increasing concern over the potential use of smallpox virus as a biol. weapon. Here, we report a high-throughput screening for anti-smallpox virus drugs from a 767-small-mol. library, employing two vaccinia virus (VACV) strains containing firefly luciferase (VTT-Fluc and VG9-Fluc) as surrogate viruses. Using an eight-point dose response format assay, 26 compounds of different pharmacol. classes were identified with in vitro anti-VACV activities. Mycophenolate mofetil (MMF) and tranilast (TRA) were detected to possess the highest anti-VACV potency (selectivity index values of >334 and >74, resp.); they could inhibit VTT-Fluc replication in nude mice at 5 days post-infection by 99% (10 mg/kg, P < .01) and 59% (45 mg/kg, P = .01), resp., as indicated by bioluminescent intensity. In conclusion, MMF and TRA are promising anti-smallpox virus candidates for further optimization and repurposing for use in clin. practice. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Related Products of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Related Products of 53902-12-8

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

Novel role for tranilast in regulating NLRP3 ubiquitination, vascular inflammation, and atherosclerosis was written by Chen, Suwen;Wang, Yadong;Pan, Yamu;Liu, Yao;Zheng, Shuang;Ding, Ke;Mu, Kaiyu;Yuan, Ye;Li, Zhaoyang;Song, Hongxian;Jin, Ying;Fu, Jian. And the article was included in Journal of the American Heart Association in 2020.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

Aberrant activation of the NLRP3 (nucleotide-binding oligomerization domain, leucine-rich repeat-containing receptor family pyrin domain-containing 3) inflammasome is thought to play a causative role in atherosclerosis. NLRP3 is kept in an inactive ubiquitinated state to avoid unwanted NLRP3 inflammasome activation. This study aimed to test the hypothesis that pharmacol. manipulating of NLRP3 ubiquitination blunts the assembly and activation of the NLRP3 inflammasome and protects against vascular inflammation and atherosclerosis. Since genetic studies yielded mixed results about the role for this inflammasome in atherosclerosis in low-d. lipoprotein receptor- or apolipoprotein E-deficient mice, this study attempted to clarify the discrepancy with the pharmacol. approach using both models. We provided the first evidence demonstrating that tranilast facilitates NLRP3 ubiquitination. We showed that tranilast restricted NLRP3 oligomerization and inhibited NLRP3 inflammasome assembly. Tranilast markedly suppressed NLRP3 inflammasome activation in low-d. lipoprotein receptor- and apolipoprotein E-deficient macrophages. Through reconstitution of the NLRP3 inflammasome in human embryonic kidney 293T cells, we found that tranilast directly limited NLRP3 inflammasome activation. By adopting different regimens for tranilast treatment of low-d. lipoprotein receptor- and apolipoprotein E-deficient mice, we demonstrated that tranilast blunted the initiation and progression of atherosclerosis. Mice receiving tranilast displayed a significant reduction in atherosclerotic lesion size, concomitant with a pronounced decline in macrophage content and expression of inflammatory mols. in the plaques compared with the control group. Moreover, tranilast treatment of mice substantially hindered the expression and activation of the NLRP3 inflammasome in the atherosclerotic lesions. Tranilast potently enhances NLRP3 ubiquitination, blunts the assembly and activation of the NLRP3 inflammasome, and ameliorates vascular inflammation and atherosclerosis in both low-d. lipoprotein receptor- and apolipoprotein E-deficient mice. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

Drug repositioning of tranilast to sensitize a cancer therapy by targeting cancer-associated fibroblast was written by Ochi, Kosuke;Suzawa, Ken;Thu, Yin Min;Takatsu, Fumiaki;Tsudaka, Shimpei;Zhu, Yidan;Nakata, Kentaro;Takeda, Tatsuaki;Shien, Kazuhiko;Yamamoto, Hiromasa;Okazaki, Mikio;Sugimoto, Seiichiro;Shien, Tadahiko;Okamoto, Yoshiharu;Tomida, Shuta;Toyooka, Shinichi. And the article was included in Cancer Science in 2022.Synthetic Route of C18H17NO5 This article mentions the following:

Cancer-associated fibroblasts (CAFs) are a major component of the tumor microenvironment that mediate resistance of cancer cells to anticancer drugs. Tranilast is an antiallergic drug that suppresses the release of cytokines from various inflammatory cells. In this study, we investigated the inhibitory effect of tranilast on the interactions between non-small cell lung cancer (NSCLC) cells and the CAFs in the tumor microenvironment. Three EGFR-mutant NSCLC cell lines, two KRAS-mutant cell lines, and three CAFs derived from NSCLC patients were used. To mimic the tumor microenvironment, the NSCLC cells were cocultured with the CAFs in vitro, and the mol. profiles and sensitivity to mol. targeted therapy were assessed. Crosstalk between NSCLC cells and CAFs induced multiple biol. effects on the NSCLC cells both in vivo and in vitro, including activation of the STAT3 signaling pathway, promotion of xenograft tumor growth, induction of epithelial-mesenchymal transition (EMT), and acquisition of resistance to mol.-targeted therapy, including EGFR-mutant NSCLC cells to osimertinib and of KRAS-mutant NSCLC cells to selumetinib. Treatment with tranilast led to inhibition of IL-6 secretion from the CAFs, which, in turn, resulted in inhibition of CAF-induced phospho-STAT3 upregulation. Tranilast also inhibited CAF-induced EMT in the NSCLC cells. Finally, combined administration of tranilast with mol.-targeted therapy reversed the CAF-mediated resistance of the NSCLC cells to the mol.-targeted drugs, both in vitro and in vivo. Our results showed that combined administration of tranilast with mol.-targeted therapy is a possible new treatment strategy to overcome drug resistance caused by cancer-CAF interaction. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Synthetic Route of C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Synthetic Route of C18H17NO5

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

The key role of organic anion transporter 3 in the drug-drug interaction between tranilast and methotrexate was written by Wang, Jingjing;Yuan, Wenjing;Shen, Qingqing;Wu, Qipeng;Jiang, Zhenzhou;Wu, Wei;Zhang, Luyong;Huang, Xin. And the article was included in Journal of Biochemical and Molecular Toxicology in 2022.Synthetic Route of C18H17NO5 This article mentions the following:

Tranilast, N-(3,4-dimethoxycinnamoyl)-anthranilic acid, is an anti-allergic drug and is considered for use in the treatment of rheumatoid arthritis. Methotrexate, an antimetabolite and folate antagonist to treat some cancers, is also a first-line drug for RA. The aim of this study was to understand whether tranilast could inhibit renal uptake transporters (Oat1, Oat3, and Oct2) and whether MTX combined with TL would have drug-drug interactions. The results of kidney slices and HEK293T-OAT3 cell uptake experiments showed that TL (10μM) could inhibit the uptake of penicillin G and MTX, which are substrates of OAT3. When TL (10 mg/kg) was combined with MTX (5 mg/kg), the area under the curve and peak concentration of MTX increased by 46.46% and 113.51%, respectivley, while the pharmacokinetic process of tranilast (10 mg/kg) was not changed by methotrexate (5 mg/kg). TL could increase plasma exposure of MTX by inhibiting Oat3 in vitro and in vivo. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Synthetic Route of C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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.Synthetic Route of C18H17NO5

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