1. GPCR/G Protein
  2. Glucocorticoid Receptor
  3. Exicorilant

Exicorilant (Synonyms: CORT 125281)

目录号: HY-117880 纯度: 99.89%
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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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥4540 In-stock
1 mg ¥1800 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
25 mg ¥9900 In-stock
50 mg ¥16500 In-stock
100 mg ¥22500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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%).
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (424.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6962 mL 8.4809 mL 16.9618 mL
5 mM 0.3392 mL 1.6962 mL 3.3924 mL
10 mM 0.1696 mL 0.8481 mL 1.6962 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.53 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.53 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

ExicorilantCORT 125281CORT125281CORT-125281Glucocorticoid ReceptorInhibitorinhibitorinhibit

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产品名称:
Exicorilant
目录号:
HY-117880
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