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首页-小分子抑制剂&激动剂-GPCR-GPR109A (Niacin Receptor 1)-MK-6892
MK-6892

Chemical Structure : MK-6892

CAS No.: 917910-45-3

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MK-6892 (MK 6892, MK6892)

货号: PC-42694Not For Human Use, Lab Use Only.

MK-6892 is a potent and selective high affinity niacin receptor (GPR109A) full agonist with Ki of 4.0 nM, EC50 of 16 nM in GTPγS assay.

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5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-6892 is a potent and selective high affinity niacin receptor (GPR109A) full agonist with Ki of 4.0 nM, EC50 of 16 nM in GTPγS assay.
MK-6892 has no activity on closely related GPCRs GPR109B and GPR81.
MK-6892 displays good PK across species, remarkably clean off-target profiles, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.

物理化学性质&存储条件

分子量 386.4018
分子式 C19H22N4O5
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

1-Cyclohexene-1-carboxylic acid, 2-[[3-[3-(5-hydroxy-2-pyridinyl)-1,2,4-oxadiazol-5-yl]-2,2-dimethyl-1-oxopropyl]amino]-

参考文献

1. Shen HC, et al. J Med Chem. 2010 Mar 25;53(6):2666-70.

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