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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Cytochrome P450 (CYPs)-ODM-208
ODM-208

Chemical Structure : ODM-208

CAS No.: 2231294-96-3

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ODM-208 (Opevesostat, ODM208)

货号: PC-49349Not For Human Use, Lab Use Only.

ODM-208 (Opevesostat) is a potent, selective, orally bioavailable CYP11A1 inhibitor, inhibits the biosynthesis of pregnenolone with IC50 of 15 nM in NCI-H295R cells.

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10 mg ￥880 In stock
25 mg ￥1480 In stock
50 mg ￥2180 In stock
100 mg ￥3580 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ODM-208 (Opevesostat) is a potent, selective, orally bioavailable CYP11A1 inhibitor, inhibits the biosynthesis of pregnenolone with IC50 of 15 nM in NCI-H295R cells.
ODM-208 is CYP11A1-selective, shows >1,000 selectivity over metabolising CYP enzymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4).
ODM-208 is superior in steroid hormone biosynthesis inhibition compared to the non-selective CYP inhibitors ketoconazole and etomidate.
ODM-208 displays pregnenolone production inhibition with IC50 of 108 nM and 2,167 nM with NADPH and without NADPH, respectively.
ODM-208 displays rapid, complete, durable, and reversible inhibition of the steroid hormone biosynthesis in an adrenocortical carcinoma cell model in vitro, in adult non-castrated male mice and dogs, and in patients with CRPC.
ODM-208 (2 mg/kg/day, oral) treatment causes a significant and dose-dependent decrease in the plasma cortisol and testosterone concentrations in adult non-castrated Beagle dogs.

物理化学性质&存储条件

分子量 418.508
分子式 C21H26N2O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one

参考文献

1. Mari Karimaa, et al. Mol Cancer Ther. 2022 Sep 21;MCT-22-0115.

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