Category: 53902-12-8

Examination of SOD1 aggregation modulators and their effect on SOD1 enzymatic activity as a proxy for potential toxicity was written by Malik, Ravinder;Corrales, Christian;Linsenmeier, Miriam;Alalami, Huda;Sepanj, Niki;Bitan, Gal. And the article was included in FASEB Journal in 2020.Computed Properties of C18H17NO5 This article mentions the following:

Small-mol. inhibitors of abnormal protein self-assembly are promising candidates for developing therapy against proteinopathies. Such compounds have been examined primarily as inhibitors of amyloid β-protein (Aβ), whereas testing of inhibitors of other amyloidogenic proteins has lagged behind. An important issue with screening compound libraries is that although an inhibitor suitable for therapy must be both effective and nontoxic, typical screening focuses on efficacy, whereas safety typically is tested at a later stage using cells and/or animals. In addition, typical thioflavin T (ThT)-fluorescence-based screens use the final fluorescence value as a readout, potentially missing important kinetic information. Here, we examined potential inhibitors of superoxide dismutase 1 (SOD1) using ThT-fluorescence including the different phases of fluorescence change and added a parallel screen of SOD1 activity as a potential proxy for compound toxicity. Some compounds previously reported to inhibit other amyloidogenic proteins also inhibited SOD1 aggregation at low micromolar concentrations, whereas others were ineffective. Anal. of the lag phase and exponential slope added important information that could help exclude false-pos. or false-neg. results. SOD1 was highly resistant to inhibition of its activity, and therefore, did not have the necessary sensitivity to serve as a proxy for examining potential toxicity. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Computed Properties of C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Computed Properties of C18H17NO5

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

Global trends in research of gouty arthritis over past decade: a bibliometric analysis was written by Deng, Pin;Wang, Shulong;Sun, Xiaojie;Qi, Yinze;Ma, Zhanhua;Pan, Xuyue;Liang, Huan;Wu, Junde;Chen, Zhaojun. And the article was included in Frontiers in Immunology in 2022.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

Gouty arthritis (GA), as a multifactorial disease, is characterised by intense pain, active inflammation symptoms, and swollen joints. It has utterly complex pathogenesis, of which the amount of research publications on GA has increased during the last few decades. A bibliometric anal. was carried out to investigate the trends, frontiers, and hot spots in global scientific output in GA research over the last decade. We retrieved the Science Citation Index Expanded (SCI-Expanded) of the Web of Science Core Collection (WoSCC) for publications and recorded information published from 2012 to 2021. we carried out the bibliometric anal. and visualisation anal. of the overall distribution of annual outputs, leading countries, active institutions, journals, authors, co-cited references, and keywords with the VOSviewer and CiteSpace. The impact and quality of papers were assessed using a global citation score (GCS). We retrieved 2052 articles and reviews in total. The annual number of publications (Np) related to GA research has increased during the latest decade. China published the most papers, and the USA achieved the highest H-index and number of citations (Nc). The League of European Research Universities (LERU) and Clin. Rheumatol. (Clin Rheumatol) are the most productive institutions and periodicals. The total GCS of the paper written by Kottgen, A. in 2013 was 479, ranking the first. The most common keywords were “Gout,” “hyperuricemia,” and “gouty arthritis.” This research revealed that though there was a slight fluctuation in publications related to GA, the Np raised on the whole. China was an enormous creator, and the USA was an influential nation in this domain. The top three contributor authors were Dalbeth, N., Singh, JA., and Choi, HK. There were few investigations on the treatment of GA by Chinese medicine monomer, and the “mechanism,” “pathway”, “nf- kappa-b”, “injury”, “receptor”, and “animal model” were growing research hotspots. Our research illustrated the hotspots of research and development trends in the research field of GA during the last decade. Recognition of the most critical indicators (researchers, countries, institutes, and journals for the release of GA research), hotspots in the research field of GA can be helpful for countries, scholars, and policymakers in this field to understand GA better make decisions. 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 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. 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.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

Tranilast, a Transient Receptor Potential Vanilloid 2 Channel (TRPV2) Inhibitor Attenuates Amyloid β-Induced Cognitive Impairment: Possible Mechanisms was written by Thapak, Pavan;Bishnoi, Mahendra;Sharma, Shyam Sunder. And the article was included in NeuroMolecular Medicine in 2022.SDS of cas: 53902-12-8 This article mentions the following:

Abstract: Alzheimer’s disease (AD) is associated with the accumulation of β-amyloid and leads to cognitive impairment. Numerous studies have established that neuronal calcium homeostasis is perturbed in AD. Recently, transient receptor potential vanilloid 2 (TRPV2) channels, a non-selective calcium-permeable channel, have been investigated in several diseases. However, the role of the TRPV2 channel has not been investigated in AD yet. In this study, intracerebroventricular administration of β-amyloid (10μg) to Sprague Dawley rats resulted in cognitive impairment which was evident from the assessment of cognitive tests. Also, TRPV2 mRNA and protein expression were found to be upregulated, while the expression of Ca^2+/calmodulin-dependent protein kinase II (p-CaMKII-Thr-286), glycogen synthase kinase 3β (p-GSK-3β-Ser-9), cAMP response element-binding protein (p-CREB-Ser-133), and postsynaptic d. protein 95 (PSD-95) were downregulated in the hippocampus of β-amyloid-treated animals. Even, β-amyloid-treated animals showed upregulation of mRNA level of calcium buffering proteins (parvalbumin and calsequestrin) and calcineurin A (PPP3CA) in the hippocampus. Acetylcholinesterase activity was also increased in the cortex of β-amyloid-treated animals. Three-week treatment with tranilast showed improvement in the cognitive parameters which was associated with a decrease in TRPV2 expression and AChE activity. Addnl., an increase in the protein expression of p-CaMKII, p-GSK-3β, p-CREB and PSD-95 in the hippocampus was found. Downregulation in the mRNA level of calcium buffering proteins (parvalbumin and calsequestrin) and calcineurin A in the hippocampus was also seen. These results reveal the importance of TRPV2 channels in the β-amyloid-induced cognitive deficits and suggest TRPV2 as a potential target for AD. 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. 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.SDS of cas: 53902-12-8

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

Protective effects of tranilast on experimental colitis in rats was written by Seto, Yoshiki;Kato, Kouki;Tsukada, Ryota;Suzuki, Hiroki;Kaneko, Yuuki;Kojo, Yoshiki;Sato, Hideyuki;Onoue, Satomi. And the article was included in Biomedicine & Pharmacotherapy in 2017.Product Details of 53902-12-8 This article mentions the following:

The present study aimed to verify the efficacy of tranilast (TL) for treating inflammatory bowel disease (IBD) with the use of an exptl. colitis model. The exptl. colitis model was prepared by intrarectal instillation of 2,4,6-trinitrobenzenesulfonic acid (TNBS; 40 mg/kg) dissolved in water containing 25% ethanol. The pharmacol. effects of TL after repeated oral administration were evaluated by biomarker and histol. analyses, and the pharmacokinetic behavior of TL was also examined after single oral administration. The intrarectal instillation of TNBS solution caused colitis, as evidenced by ca. 2.2-, 5-, and 3-fold increases in myeloperoxidase (MPO) activity, infiltrated cell numbers, and the thickness of the submucosa in the colon, resp. However, orally-taken TL (10 mg/kg, twice a day for 9 days) led to a 92% reduction in the increase of the MPO level by TNBS enema, and cellular infiltration and thickened submucosa in the exptl. colitis model tended to also be suppressed by repeated oral administration of TL. The oral bioavailability of TL in TNBS-treated rats was calculated to be as low as ca. 6.5%, and the poor oral absorption of TL may be a limitation of the treatment for IBD. TL could attenuate TNBS-induced colitis on the basis of the obtained results, and the anti-inflammatory effects would have clin. relevance to the therapeutic outcomes of TL in IBD patients. Although further improvement in the oral bioavailability of TL might be required for better pharmacol. outcomes, TL would be an efficacious agent for treating IBD. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Product Details of 53902-12-8).

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

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

Tranilast ameliorated subchronic silver nanoparticles-induced cerebral toxicity in rats: Effect on TLR4/NLRP3 and Nrf-2 was written by Fahmy, Eslam K.;El-Sherbiny, Mohamed;Said, Eman;Elkattawy, Hany A.;Qushawy, Mona;Elsherbiny, Nehal. And the article was included in NeuroToxicology in 2021.COA of Formula: C18H17NO5 This article mentions the following:

Silver nanoparticles (AgNPs) are widely applied in various aspects of life. However, recent studies reported their potential toxicity both on environment and human health. The present study aimed to unravel the underlying mol. mechanisms involved in AgNPs-induced brain toxicity. Moreover, chemopreventive effect of tranilast, an analog of tryptophan metabolite and a mast cell membrane stabilizer was evaluated. Thirty Sprague Dawley rats were enrolled equally into Normal control group, AgNPs-intoxicated group (50 mg/kg, 3 times/wk) and tranilast (300 mg/kg, 3 times/wk)+AgNPs group. AgNPs administration triggered brain oxidative stress as depicted by reduced Nrf-2 expression, decreased TAC and GSH as well as upregulated brain lipid peroxidation The apparent brain oxidative damage was accompanied by elevated levels of inflammatory cytokines (IL-β1;, IL-6 and TNF-α). Moreover, brain levels of TLR4, NLRP3 and caspase-1 were up-regulated. Addnl., histol. study indicated marked cellular injury in cerebrum and cerebellum specimens. This was concomitant with elevated serum CK activity and CK-BB level. On the other hand, tanilast administration remarkably alleviated AgNPs-induced brain toxicity. The present study shed the light on implication of TLR4/NLRP3 axis and NrF2 in AgNPs-induced brain toxicity. In addition, it explored the potential protective effect of tranilast on AgNPs-induced brain injury via antioxidant and anti-inflammatory efficacies. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8COA of Formula: 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. 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.COA of Formula: C18H17NO5

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

[Effect of tranilast on wound healing and administration time on scar hyperplasia of deep partial-thickness burn in mice]. was written by Hu, Zhenzhen;Chen, Bin;Li, Yang;Jiang, Wei;Wen, Lihong;Ji, Fukang;Yang, Xiao;Wang, Jinhuang;Liu, Dalie. And the article was included in Zhongguo xiu fu chong jian wai ke za zhi = Zhongguo xiufu chongjian waike zazhi = Chinese journal of reparative and reconstructive surgery in 2017.Product Details of 53902-12-8 This article mentions the following:

Objective: To investigate the effect of tranilast on wound healing and the mechanism of inhibiting scar hyperplasia in mice, and to study the relationship between the inhibiting ability of tranilast on scar hyperplasia and administration time. Methods: Sixty-six Kunming mice were selected to build deep II degree burn model, and were randomly divided into the control group (18 mice), the early intervention group (18 mice), the medium intervention group (18 mice), and the late intervention group (12 mice). The mice in the early intervention group, the medium-term intervention group, and the late intervention group were given tranilast 200 mg/(kg·d) by gastrogavage at immediate, 7 days, and 14 days after burn respectively, and the mice in the control group were managed with same amount of normal saline every day. The wound healing was observed regularly. At 14, 28, and 42 days in the early and medium intervention groups and at 28 and 42 days in the late intervention group, fresh tissues were taken from 6 mice to observe the shape of mast cells by toluidine blue staining, collagen content by Masson staining; the collagen type I and collagen type III content were measured to calculate the I/III collagen content ratio by immunohistochemistry method, the contents of transforming growth factor β ₁ (TGF-β ₁) and histamine were detected by ELISA; and the ultrastructure of fibroblasts was observed under transmission electron microscope. Results: There was no significant difference in wound healing time between groups ( F=1.105, P=0.371). The mast cells number, collagen content, TGF-β ₁ content, histamine content, and the I/III collagen content ratio in the early intervention group were significantly less than those in the other groups ( P<0.05). Significant difference was found in mast cells number, collagen content, and histamine content between control group and medium or late intervention group at the other time points ( P<0.05) except between control group and late intervention group at 42 days ( P>0.05). Compared with the control group, the activity of fibroblasts in the early intervention group was obviously inhibited, and the arrangement of the fibers was more regular; the fibroblast activity in the medium and late intervention groups was also inhibited obviously. Conclusion: Tranilast has no obvious effect on the wound healing time in mice. Tranilast intervention shows the inhibitory effect on the scar hyperplasia which can significantly reduce the number of mast cells, the content of histamine and TGF-β ₁, inhibit the ability of fibroblasts synthetic collagen and adjust the proportion of collagen synthesis. The immediate tranilast intervention may have the best inhibitory effect on scar hyperplasia. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Product Details of 53902-12-8).

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 can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Product Details of 53902-12-8

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

Combining Theoretical and Data-Driven Approaches To Predict Drug Substance Hydrate Formation was written by Tilbury, Carl J.;Chen, Jie;Mattei, Alessandra;Chen, Shuang;Sheikh, Ahmad Y.. And the article was included in Crystal Growth & Design in 2018.HPLC of Formula: 53902-12-8 This article mentions the following:

Hydrates represent a very significant fraction of pharmaceutical mol. crystals and can be leveraged to simplify downstream processing for formulations such as wet granulation and hot-melt extrusion. In silico methods to predict hydrate formation can guide exptl. screening and evaluate residual risk of selected forms. Both solution mixing thermodn. and relative propensities of hydrogen bond formation can be used for virtual screening. Our study assessed these techniques for a previously studied set of relatively simple drug compounds (average mol. weight 300) and a new set of more complex AbbVie-pipeline compounds (average mol. weight 550). Although solution thermodn. have been shown to successfully discriminate hydrate formation for the set of smaller drug mols., this technique did not provide successful screening for the more complex set of AbbVie compounds tested. A single-differential hydrogen bond propensity (SD-HBP) score, which accounts for only the strongest donor-acceptor pairing in both anhydrate and hydrate forms, also provides little utility. We therefore developed a multi-differential hydrogen bond propensity (MD-HBP) score that considers the competitive effect of multiple donor-acceptor interactions in each form. Addnl., the MD-HBP score utilizes COSMO-RS theory to predict solid-state conformations, to strengthen the data-driven anal. of the solid-state and ensure more accurate description of possible hydrogen bond networks in anhydrate and hydrate solid forms. This quant. MD-HBP score performed well at differentiating between hydrate-forming and non-hydrate-forming compounds for both sets of compounds; thus, it can be applied more broadly in solid form development. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8HPLC of Formula: 53902-12-8).

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

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

Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors was written by Yokoyama, Takeshi;Kashihara, Mirai;Mizuguchi, Mineyuki. And the article was included in Journal of Medicinal Chemistry in 2021.Formula: C18H17NO5 This article mentions the following:

Transthyretin (TTR) is a causative protein of TTR amyloidosis (ATTR amyloidosis), a general term for diseases characterized by deposition of TTR amyloid fibrils in specific organs. ATTR amyloidosis can be ameliorated by stabilization of the TTR tetramer through the binding of small mols. Here, we show that the clin. anthelmintic drugs bithionol (42) and triclabendazole (43) potently inhibit aggregation of the amyloidogenic variant V30M-TTR. A competitive binding assay using a fluorescence probe showed that the binding affinity of 42 with V30M-TTR was significantly higher than that of the first-in-class drug tafamidis (1), and the binding affinity of 43 was similar to that of 1. The crystallog. and thermodn. anal. revealed that 42 efficiently occupied the halogen-binding grooves of TTR, resulting in the favorable binding entropy. Multifaceted in vitro studies of anthelmintic drugs have the potential to reposition these drugs as ATTR amyloidosis inhibitors. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Formula: 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. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Formula: C18H17NO5

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

Prediction of permeability across intestinal cell monolayers for 219 disparate chemicals using in vitro experimental coefficients in a pH gradient system and in silico analyses by trivariate linear regressions and machine learning was written by Kamiya, Yusuke;Omura, Asuka;Hayasaka, Riku;Saito, Rie;Sano, Izumi;Handa, Kentaro;Ohori, Junya;Kitajima, Masato;Shono, Fumiaki;Funatsu, Kimito;Yamazaki, Hiroshi. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2021.Related Products of 53902-12-8 This article mentions the following:

For medicines, the apparent membrane permeability coefficients (Papp) across human colorectal carcinoma cell line (Caco-2) monolayers under a pH gradient generally correlate with the fraction absorbed after oral intake. Furthermore, the in vitro Papp values of 29 industrial chems. were found to have an inverse association with their reported no-observed effect levels for hepatotoxicity in rats. In the current study, we expanded our influx permeability predictions for the 90 previously investigated chems. to both influx and efflux permeability predictions for 207 diverse primary compounds, along with those for 23 secondary compounds Trivariate linear regression anal. found that the observed influx and efflux logPapp values determined by in vitro experiments significantly correlated with mol. weights and the octanol-water distribution coefficients at apical and basal pH levels (pH 6.0 and 7.4, resp.) (apical to basal, r = 0.76, n = 198; and basal to apical, r = 0.77, n = 202); the distribution coefficients were estimated in silico. Further, prediction accuracy was enhanced by applying a light gradient boosting machine learning system (LightGBM) to estimate influx and efflux logPapp values that incorporated 17 and 19 in silico chem. descriptors (r = 0.83-0.84, p < 0.001). The determination in vitro and/or prediction in silico of permeability coefficients across intestinal cell monolayers of a diverse range of industrial chems./food components/medicines could contribute to the safety evaluations of oral intakes of general chems. in humans. Such new alternative methods could also reduce the need for animal testing during toxicity assessment. 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. 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. 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.Related Products of 53902-12-8

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

Aloe-emodin, a naturally occurring anthraquinone, is a highly potent mast cell stabilizer through activating mitochondrial calcium uniporter was written by Gao, Yuan;Zhang, Xiaoyu;Li, Ximeng;Qi, Ruijuan;Han, Yixin;Kang, Yuan;Cai, Runlan;Peng, Cheng;Qi, Yun. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2021.Product Details of 53902-12-8 This article mentions the following:

Mast cells play a fundamental role in immune system. Upon stimulation, they are activated via IgE dependent or independent pathway and then release granules which contain plenty of preformed constituents. Mast cell stabilizers are commonly used clin. for inhibiting the degranulation of mast cells. In the current study, we firstly identified aloe-emodin, a naturally occurring anthraquinone, was a prominent mast cell stabilizer. It could strikingly dampen IgE/FcεRI- and MAS-related G protein coupled receptor (Mrgpr)-mediated mast cell degranulation in vitro and in vivo. Mechanism study indicated that aloe-emodin rapidly and reversibly decreased cytosolic Ca2+ (Ca2+[c]) concentration through enhancing the mitochondrial Ca2+ (Ca2+[m]) uptake. After genetically silencing or pharmacol. inhibiting mitochondrial calcium uniporter (MCU), the effects of aloe-emodin on the Ca2+[c] level and mast cell degranulation were significantly weakened. In contrast to six clin. drugs with mast cell stabilizing properties (amlexanox, tranilast, ketotifen, cromolyn disodium salt, dexamethasone and pimecrolimus), aloe-emodin showed an impressive and potent inhibitory action on the mast cell degranulation. Collectively, aloe-emodin is a highly potent mast cell stabilizer. By directly activating MCU, it decreases Ca2+[c] level to suppress mast cell degranulation. Our study may provide a promising candidate for the treatment of mast cell activation-related diseases. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Product Details of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Product Details of 53902-12-8

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