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首页-小分子抑制剂&激动剂-GPCR-Melanocortin Receptor-BMS-470539 dihydrochloride
BMS-470539 dihydrochloride

Chemical Structure : BMS-470539 dihydrochloride

CAS No.: 2341796-82-3

BMS-470539 dihydrochloride (BMS470539)

货号: PC-60215Not For Human Use, Lab Use Only.

BMS-470539 dihydrochloride is a potent, selective, full agonist of human and murine melanocortin-1 receptor (MC-1R) with EC50 of 16.8 and 11.6 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BMS-470539 dihydrochloride is a  potent, selective, full agonist of human and murine melanocortin-1 receptor (MC-1R) with EC50 of 16.8 and 11.6 nM, respectively.
BMS-470539 dose-dependently inhibits TNFα-induced activation of a NF-kappaB transcriptional reporter in human melanoma cells.
BMS-470539 inhibits LPS-induced TNFα production in BALB/c mice (EC50=10 uM/kg).
BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature.

物理化学性质&存储条件

分子量 632.63
分子式 C32H43Cl2N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-2-amino-N-((R)-1-(4-butyryl-4-phenylpiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl)-3-(1-methyl-1H-imidazol-5-yl)propanamide dihydrochloride

参考文献

1. Kang L, et al. J Leukoc Biol. 2006 Oct;80(4):897-904.

2. Leoni G, et al. Br J Pharmacol. 2010 May;160(1):171-80.

3. Doyle JR, et al. J Pharmacol Exp Ther. 2012 Aug;342(2):318-26.

4. Herpin TF, et al. J Med Chem. 2003 Mar 27;46(7):1123-6.

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