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BMS 493
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS 493图片
CAS NO:215030-90-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
BMS 493 是一种反向泛视黄酸受体 (RAR) 激动剂。
Cas No.215030-90-3
别名BMS 204493
化学名(E)-4-(2-(5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid
Canonical SMILESOC(C1=CC=C(C=C1)/C=C/C2=CC=C3C(C)(C)CC=C(C#CC4=CC=CC=C4)C3=C2)=O
分子式C29H24O2
分子量404.5
溶解度25mg/mL in DMSO, 30mg/mL in DMF
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BMS493 is an inverse agonist of pan-retinoic acid receptors (pan-RARs). This compound has been shown to increase nuclear corepressor (NCoR) interaction with RARs.

The retinoic acid receptor (RAR), a type of nuclear receptor , is a ligand-dependent transcription factor that is activated by 9-cis retinoic acid and all-trans retinoic acid. Binding of agonist ligands to RAR results in dissociation of corepressor and recruitment of coactivator protein that, in turn, promotes transcription of the downstream target gene into mRNA and eventually protein. This protein controls a number of physiological processes including cell growth, differentiation, survival, and death.

In cellular culture, pretreatment of BMS493 on MEPM cells blocked atRA-induced apoptotic indexes. Mechanistically, this component completely inhibited atRA-induced Sub-G1 fraction, DNA fragmentation, and caspase-3 activation.1.

In vivo, inhibition of RAR signaling with BMS493 induced a very high degree of congenital diaphragmatic hernia, which was associated with a marked left–right sidedness that depended on the timing of drug delivery2.

References:
1. Yu Z, Han J, Lin J, et al. Apoptosis induced by atRA in MEPM cells is mediated through activation of caspase and RAR. Toxicological sciences : an official journal of the Society of Toxicology. 2006;89(2):504-509.
2. Clugston RD, Zhang W, Alvarez S, et al. Understanding abnormal retinoid signaling as a causative mechanism in congenital diaphragmatic hernia. American journal of respiratory cell and molecular biology. 2010;42(3):276-285.