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Relacorilant

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Purity:99%

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COA HNMR HPLC

Relacorilant

Catalog No. T16727Cas No. 1496510-51-0

Relacorilant is a selective and orally bioavailable antagonist of glucocorticoid receptor(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 the potential for Cushing’s syndrome treatment.

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Pack Size	Price	Availability
1 mg	$113	In Stock
5 mg	$282	In Stock
10 mg	$448	In Stock
25 mg	$747	In Stock
50 mg	$1,050	In Stock
100 mg	$1,420	In Stock
1 mL x 10 mM (in DMSO)	$358	In Stock

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Product Introduction

Bioactivity

Description	Relacorilant is a selective and orally bioavailable antagonist of glucocorticoid receptor(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 the potential for Cushing’s syndrome treatment.
In vitro	Relacorilant also displays effective inhibition on CYP2C8 and CYP3A4 (IC50s, 0.21, 1.3 μM, respectively). It also modestly inhibits CYP2C9, 2C19, 2D6, and 3A5 (ICC50s: 2, 8, 9, and 4.9 μM, respectively)[1].
In vivo	Relacorilant (30 mg/kg, p.o., twice a day) obviously blocks the effects on plasma insulin. It fully inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing’s syndrome, and a similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day [1].
Alias	CORT 125134

Chemical Properties

Molecular Weight	586.56
Formula	C27H22F4N6O3S
Cas No.	1496510-51-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (38.36 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7049 mL	8.5243 mL	17.0486 mL	85.2428 mL
5 mM	0.3410 mL	1.7049 mL	3.4097 mL	17.0486 mL
10 mM	0.1705 mL	0.8524 mL	1.7049 mL	8.5243 mL
20 mM	0.0852 mL	0.4262 mL	0.8524 mL	4.2621 mL

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