BMS-470539 dihydrochloride|cas:2341796-82-3|西域试剂

BMS-470539 dihydrochloride,99.95%

产品编号：Bellancom-115644| CAS NO：2341796-82-3| 分子式：C₃₂H₄₃Cl₂N₅O₄| 分子量：632.62

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-115644	￥1800.00	杭州北京（现货）
Bellancom-115644	￥2800.00	杭州北京（现货）
Bellancom-115644	￥6300.00	杭州北京（现货）
Bellancom-115644	￥11500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

BMS-470539 dihydrochloride

产品介绍

BMS-470539 dihydrochloride 是一种高效的选择性黑皮质素 1 受体 (MC-1 R) 激动剂，IC₅₀ 为 120 nM，EC₅₀ 为 28 nM。BMS-470539 dihydrochloride 不激活 MC-3R，并且对 MC-4R 和 MC-5R 的激活活性非常弱。BMS-470539 dihydrochloride 具有强效的抗炎特性。

生物活性

BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC₅₀ of 120 nM, an EC₅₀ of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties.

体外研究

An HBL melanoma cell line is established that stably expresses a NF-κB luciferase reporter. In these cells, 0.5 ng/mL TNF-α induces a dose-dependent increase in NF-κB luciferase activity. Treatment of HBL-NF-κB cells with BMS-470539 elicits a dose-dependent, statistically significant reduction in TNF-α-stimulated NF-κB luciferase activity. BMS-470539 has no effect on luciferase reporter activity in the absence of TNF-α stimulation. In nontransfected HBL cells, treatment with BMS-470539 results in a dose-dependent inhibition of NF-B nuclear translocation.

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

体内研究

BMS-470539 (2.05-18.47 mg/kg; intravenous injection; for 125 minutes; WT and MC1 receptor recessive e/e mice) treatment inhibits cell adhesion and emigration with no effect on cell rolling. And also inhibits the tissue expression of both CXCL1 and CCL2.

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

Animal Model:	Wild-type (WT) and MC1 receptor recessive e/e mice induced with ischaemia-reperfusion
Dosage:	2.05 mg/kg, 6.16 mg/kg and 18.47 mg/kg
Administration:	Intravenous injection; for 125 minutes
Result:	Inhibited cell adhesion and emigration with no effect on cell rolling. Inhibited tissue expression of both CXCL1 and CCL2.

体内研究

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

Animal Model:	Wild-type (WT) and MC1 receptor recessive e/e mice induced with ischaemia-reperfusion
Dosage:	2.05 mg/kg, 6.16 mg/kg and 18.47 mg/kg
Administration:	Intravenous injection; for 125 minutes
Result:	Inhibited cell adhesion and emigration with no effect on cell rolling. Inhibited tissue expression of both CXCL1 and CCL2.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 125 mg/mL (197.59 mM)

H₂O : ≥ 100 mg/mL (158.07 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5807 mL	7.9036 mL	15.8073 mL
5 mM	0.3161 mL	1.5807 mL	3.1615 mL
10 mM	0.1581 mL	0.7904 mL	1.5807 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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献