1. GPCR/G Protein
  2. Glucocorticoid Receptor

Exicorilant (Synonyms: CORT 125281)

目录号: HY-117880
产品使用指南

Exicorilant (CORT 125281) 是选择性的、并具有口服活性的糖皮质激素受体 (GR) 的拮抗剂,其 Ki 值为 7 nM。Exicorilant (CORT 125281) 具有克服肥胖、葡萄糖不耐受和血脂异常的潜能。

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Exicorilant Chemical Structure

Exicorilant Chemical Structure

CAS No. : 1781244-77-6

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Description

Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM[1]. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia[2].

IC50 & Target

Ki: 7 nM (GR)[1].

In Vitro

Exicorilant (CORT 125281) reverses corticosterone-mediated GR activity in murine brown adipocytes in vitro[1].

In Vivo

Exicorilant (CORT 125281) reduces body weight, fat mass and plasma lipids in HFD-fed mice[2].
Exicorilant (CORT 125281) (6, 20 or 60 mg/kg/d, for 3 weeks in mice) at different dosages reduce body weight, fat mass, plasma TG, cholesterol and FFA in a dose-dependent manner, with no effect on lean mass[2].

Animal Model: Ten-week old male C57BL/6J mice HFD-fed[2].
Dosage: 6, 20, 60 mg/kg.
Administration: Orally mixed with food daily for 3 weeks.
Result: Reduced HFD-induced body weight gain with approximately 10% for CORT125281 at d21.
Significantly lowered plasma TG (-56%) and cholesterol levels (-30%).
References
Molecular Weight

589.56

Formula

C₂₆H₂₃F₄N₇O₃S

CAS No.

1781244-77-6

SMILES

O=C([C@]12CC3=C(N(C4=CC=C(F)C=C4)N=C3)C[C@]1([H])CCN(S(=O)(C5=NN(C)N=C5)=O)C2)C6=NC=CC(C(F)(F)F)=C6

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
Exicorilant
目录号:
HY-117880
需求量:

Exicorilant

Cat. No.: HY-117880