OP-3633
目录号 : GC36809OP-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
Sample solution is provided at 25 µL, 10mM.
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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.
Cas No. | 2102494-14-2 | SDF | |
Canonical SMILES | O=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 |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.244 mL | 11.2198 mL | 22.4396 mL |
5 mM | 0.4488 mL | 2.244 mL | 4.4879 mL |
10 mM | 0.2244 mL | 1.122 mL | 2.244 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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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.PMID:31274313DOI:10.1021/acs.jmedchem.9b00711
Structure-based modification of mifepristone (1) led to the discovery of novel mifepristone derivatives with improved selectivity profile. Addition of a methyl group at the C10 position of the steroid has a significant impact on progesterone receptor (PR) and androgen receptor (AR) activity. Within this series, OP-3633 (15) emerged as a glucocorticoid receptor (GR) antagonist with increased selectivity against PR and AR, improved cytochrome P450 inhibition profile, and significantly improved pharmacokinetic properties compared to 1. Furthermore, 15 demonstrated substantial inhibition of GR transcriptional activity in the GR positive HCC1806 triple negative breast cancer xenograft model. Overall, compound 15 is a promising GR antagonist candidate to clinically evaluate the impact of GR inhibition in reversal or prevention of therapy resistance.