Relacorilant(CORT 125134)

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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。

CAS NO:

1496510-51-0

包装与价格：

包装	价格(元)
250mg	电议
500mg	电议

产品介绍

Relacorilant是一种有效的，选择性的，可口服的糖皮质激素受体(glucocorticoidreceptor)拮抗剂，在HepG2TAT实验中，Ki值为7.2nM，在细胞体系中，对大鼠，人和猴子糖皮质激素受体的Ki值分别为12，81.2，210nM；Relacorilant已经进入临床2期来研究库欣综合征。

Cas No.	1496510-51-0
Canonical SMILES	O=C(C1=CC(C(F)(F)F)=CC=N1)[C@@]2(CN(S(=O)(C3=CN(C)N=C3)=O)CC4)C4=CC5=C(C=NN5C6=CC=C(F)C=C6)C2
分子式	C₂₇H₂₂F₄N₆O₃S
分子量	586.56
溶解度	Soluble in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively; Relacorilant has entered phase 2 clinical study in patients with Cushing's syndrome. Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant also shows potent inhibition on CYP2C8 and CYP3A4 (IC50s, 0.21, 1.3 μM, respectively), modestly inhibits CYP2C9, 2C19, 2D6 and 3A5, with ICC50s of 2, 8, 9, and 4.9 μM, respectively[1]. Relacorilant (30 mg/kg, p.o., twice a day) dramaticlly blocks the effects on plasma insulin and completely inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing's syndrome, and similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day[1]. [1]. Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421.