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首页-小分子抑制剂&激动剂-GPCR-GPR109A (Niacin Receptor 1)-MK-0354
MK-0354

Chemical Structure : MK-0354

CAS No.: 851776-28-8

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MK-0354 (MK0354)

货号: PC-43317Not For Human Use, Lab Use Only.

MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1880 In stock
25 mg ￥3280 In stock
50 mg ￥5280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays.
MK-0354 shows no interaction with any other target in a panel of over 120 other proteins.
MK-0354 is a competitive inhibitor of 3H-nicotinic acid binding to hGPR109a with Ki of 505 nM, fully inhibits isoproterenol stimulated lipolysis in human adipocytes with IC50 of 3.1 uM.
MK-0354 also is a competitive antagonist of nicotinic acid-induced MAPK signaling in cells overexpressing either mGPR109a or hGPR109a.
MK-0354 possesses plasma FFA lowering effects in mice comparable to those of nicotinic acid, does not induce vasodilation.

物理化学性质&存储条件

分子量 176.1786
分子式 C7H8N6
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

DMSO: ≥ 36 mg/mL
Chemical Name/SMILES

Cyclopentapyrazole, 1,4,5,6-tetrahydro-3-(2H-tetrazol-5-yl)-

参考文献

1. Semple G, et al. J Med Chem. 2008 Aug 28;51(16):5101-8.

2. Lai E, et al. J Clin Lipidol. 2008 Oct;2(5):375-83.

3. Walters RW, et al. J Clin Invest. 2009 May;119(5):1312-21.

4. Gaidarov I, et al. Cell Signal. 2013 Oct;25(10):2003-16.

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