产品名称

Osilodrostat (LCI699)

一般描述

Osilodrostat (LCI699) is a potent inhibitor of 11β-hydroxylase, an enzyme catalyzing the final step of cortisol synthesis.

别 称

4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile

纯 度

≥98.5%(HPLC)

CAS NO.

928134-65-0

分子式

C¹³H¹⁰FN³

分子量

227.24

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥35mg/ml

乙醇

≥35mg/ml

水

≥5mg/ml

l  生物学信息

生物活性/药理作用

Osilodrostat is an orally bioavailable inhibitor of both steroid 11beta-hydroxylase (cytochrome P450 (CYP) 11B1) and aldosterone synthase (CYP11B2; steroid 18-hydroxylase), with potential anti-adrenal activity and ability to treat Cushing disease (CD). Upon administration, osilodrostat binds to and inhibits the activity of CYP11B1, the enzyme that catalyzes the final step of cortisol synthesis from the precursor 11-deoxycortisol, and CYP11B2, the enzyme that catalyzes aldosterone synthesis from corticosterone and 11-deoxycorticosterone in the adrenal gland. The inhibition of CYP11B1 prevents the production of excess cortisol, thereby decreasing and normalizing the levels of cortisol. CD is most often caused by an adrenocorticotropic hormone (ACTH)-secreting  pituitary tumor.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov