| Identification | Back Directory | [Name]
MK-7246 | [CAS]
1218918-62-7 | [Synonyms]
MK-7246
CS-2898
MK7246;MK 7246
MK7246;MK 7246;MK-7246
ethyl 2-(7-(4-fluoro-N-MethylphenylsulfonaMido)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)acetate
(7R)-7-[[(4-Fluorophenyl)sulfonyl]methylamino]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-acetic acid
(R)-2-(7-(4-fluoro-N-MethylphenylsulfonaMido)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)acetic acid
2-[(7R)-7-[(4-FLUOROPHENYL)SULFONYL-METHYLAMINO]-6,7,8,9-TETRAHYDROPYRIDO[1,2-A]INDOL-10-YL]ACETIC ACID
Pyrido[1,2-a]indole-10-acetic acid, 7-[[(4-fluorophenyl)sulfonyl]methylamino]-6,7,8,9-tetrahydro-, (7R)- | [Molecular Formula]
C21H21FN2O4S | [MOL File]
1218918-62-7.mol | [Molecular Weight]
416.47 |
| Chemical Properties | Back Directory | [Boiling point ]
636.5±65.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:250.0(Max Conc. mg/mL);600.28(Max Conc. mM) | [form ]
A solid | [pka]
4.50±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MK-7246 is a potent and selective CRTH2 antagonist for the treatment of respiratory diseases. | [in vivo]
Whether the inhibition of a clinically-relevant mechanism of allergic lung inflammation such as CRTH2 will lead to a suppression of inflammatory responses is investigated in A. alternata challenged Brown Norway rats (n=8 per group). Mast cell derived production of Prostaglandin D2 (PGD2) is believed to be a prime mediator of allergic inflammation. Since CRTH2 plays an important role in the early aspects of the allergic inflammation cascade, the effect of the CRTH2 antagonist is examined on A. alternate elicited pulmonary inflammatory responses. CRTH2 inhibitor MK-7246 is orally administered 1 h before and 23 h post-intratracheal instillation of the A. alternata. MK-7246 produces a dose dependent decrease in the number of eosinophils with a maximal inhibition of 74±5% in the 100 mg/kg group (P<0.05), IL-5 (80±12%) and IL-13 (76±14%) cytokines levels (P<0.05) [2]. | [IC 50]
DP: 2.5 nM (Ki); TP: 3804 nM (Ki) | [storage]
Store at -20°C |
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