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：2102494-14-2
分子式：C30H39NO2
分子量：445.64
纯度：98%
存储：Store at -20°C

Background:

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.