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OP-3633
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。
OP-3633图片
CAS NO:2102494-14-2

OP-3633 是一种高效的甾体糖皮质激素受体 (GR) 拮抗剂,其 IC50 值为 29 nM,具有 GR 转录活性抑制作用。OP-3633 表现出极弱的孕酮受体受体 (PR) 激动作用和雄激素受体 (AR) 拮抗作用。
Cas No.2102494-14-2
Canonical SMILESO=C1CC[C@]2(C)[C@@]3([H])[C@@H](C4=CC=C(N(C)C)C=C4)C[C@]5(C)[C@@](C#CC)(O)CC[C@@]5([H])[C@]3([H])CCC2=C1
分子式C30H39NO2
分子量445.64
溶解度Soluble in DMSO
储存条件Store at -20°C
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

OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism[1]. IC50: 29 nM (GR)[1]

OP-3633 exhibits low progesterone receptor (PR) agonism with an EC50 higher than 2500 nM[1]. OP-3633 exhibits low androgen receptor (PR) antagonism, with an IC50 of 1135 nM[1].

[1]. Du X, et al. Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633). J Med Chem. 2019 Jul 25;62(14):6751-6764.

 
 
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