CLP-3094|cas:312749-73-8|西域试剂

CLP-3094,95.0%

产品编号：Bellancom-141487| CAS NO：312749-73-8| 分子式：C₁₅H₁₃ClN₂OS| 分子量：304.79

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-141487		￥1300.00	杭州北京（现货）
Bellancom-141487		￥2300.00	杭州北京（现货）

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CLP-3094

产品介绍

CLP-3094 是一种有效的雄激素受体 (AR) BF3 (binding function 3) 抑制剂。BF3-IN-1 抑制 AR 转录活性 (IC₅₀=4 μM)。CLP-3094 是一种选择性、有效的 GPR142 拮抗剂。

生物活性

CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC₅₀=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.

体外研究

CLP-3094 inhibits both an increase of intracellular Ca²⁺ concentration ([Ca²⁺]i) induced by L-tryptophan using CHO-K1 cells expressing GPR142 in the aequorin assay, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. The IC₅₀ of CLP-3094 is 0.2 μM against 200 μM L-tryptophanfor the mouse receptor and 2.3 μM against 1 mM L-tryptophan for the human receptor in the aequorin assay. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantly lower severity of arthritis scores than vehicletreated mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CAIA mouse model (Female DBA1/J mice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)
Dosage:	30, 100 mg/kg
Administration:	I.p. daily from Day 0 to Day 11
Result:	Dose-dependently reduced, by not much, the arth-ritis scores.

体内研究

CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantly lower severity of arthritis scores than vehicletreated mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CAIA mouse model (Female DBA1/J mice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)
Dosage:	30, 100 mg/kg
Administration:	I.p. daily from Day 0 to Day 11
Result:	Dose-dependently reduced, by not much, the arth-ritis scores.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (328.09 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2809 mL	16.4047 mL	32.8095 mL
5 mM	0.6562 mL	3.2809 mL	6.5619 mL
10 mM	0.3281 mL	1.6405 mL	3.2809 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: ≥ 2.5 mg/mL (8.20 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.20 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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，得到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: ≥ 2.5 mg/mL (8.20 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.20 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。