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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-MK-7246
MK-7246

Chemical Structure : MK-7246

CAS No.: 1218918-62-7

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MK-7246 (MK7246;MK-7246)

货号: PC-61565Not For Human Use, Lab Use Only.

MK-7246 is a potent, selectie, orally available prostaglandin D2 receptor (CRTH2, GPR44) antagonist with Ki of 2.5 nM (hCRTH2).

规格 价格 库存 数量
5 mg ￥2880 In stock
10 mg ￥4280 In stock
25 mg ￥7280 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-7246 is a potent, selectie, orally available prostaglandin D2 receptor (CRTH2, GPR44) antagonist with Ki of 2.5 nM (hCRTH2).
MK-7246 displayes149-fold selectivity over DP receptor, >1,500-fold over other prostanoid receptors, also binds to recombinant mouse, rat, dog and cynomolgus monkey CRTH2 receptors with Ki of <10 nM.
MK-7246 blocks DK-PGD2-induced inhibition of cAMP formation in HEK293E-CRTH2 cells with IC50 of 3 nM, inhibits DK-PGD2-induced eosinophil shape change (IC50=2.2 nM), also efficiently blocksDK-PGD2-induced CD11b up-regulation on eosinophils and basophils (IC50= 6.2 and 5.4 nM) in human whole blood.
MK-7246 significantly reduces antigen-induced late phase bronchoconstriction and airway hyper-responsiveness in vivo.

物理化学性质&存储条件

分子量 416.467
分子式 C21H21FN2O4S
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

{(7R)-7-[[(4-fluorophenyl)sulfonyl](methyl)amino]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl}acetic acid

参考文献

1. Gervais FG, et al. Mol Pharmacol. 2011 Jan;79(1):69-76.

2. Gallant M, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93.

3. Wang YH, et al. Clin Pharmacol Ther. 2012 Jul;92(1):96-102.

4. Gil MA, et al. Eur J Pharmacol. 2014 Nov 15;743:106-16.

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