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Chemical Structure : MK-7246
CAS No.: 1218918-62-7
Catalog No.: 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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $288 | In stock | |
| 10 mg | $428 | In stock | |
| 25 mg | $728 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 416.467 | |
| Formula | C21H21FN2O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
{(7R)-7-[[(4-fluorophenyl)sulfonyl](methyl)amino]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl}acetic acid |
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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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