Identification | Back Directory | [Name]
MK 0524 | [CAS]
571170-77-9 | [Synonyms]
CS-623 MK 0524 Cardaptive Laropiprant Laropiprant, >=99% Laropiprant(MK0524) MK-0524(Laropiprant)/ MK0524;LAROPIPRANT;MK-0524 [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid (R)-2-(4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (3R)-4-[(4-Chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)cyclopent[b]indole-3-acetic acid Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)- Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-Laropiprant (3R)-4-[(4-Chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)cyclopent[b]indole-3-acetic acid Laropiprant MK 0524 | [EINECS(EC#)]
682-424-1 | [Molecular Formula]
C21H19ClFNO4S | [MDL Number]
MFCD11042421 | [MOL File]
571170-77-9.mol | [Molecular Weight]
435.9 |
Chemical Properties | Back Directory | [Melting point ]
175∶C | [Boiling point ]
710.0±60.0 °C(Predicted) | [density ]
1.48 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO:20.0(Max Conc. mg/mL);45.88(Max Conc. mM) DMF:20.0(Max Conc. mg/mL);45.88(Max Conc. mM) DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.45(Max Conc. mM) Ethanol:5.0(Max Conc. mg/mL);11.47(Max Conc. mM) | [form ]
Powder | [pka]
4.54±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Definition]
ChEBI: Laropiprant is an indolyl carboxylic acid. | [Biological Activity]
MK-0524 is a potent and selective prostaglandin D2 (PGD2) receptor PTGDR (DP1) antagonist with inverse agonist activity (Ki = 570 pM/DP12.95 nM/TP745 nM/DP2>890 nM for EP1/2/3/4FP and IP). MK-0524 inhibits cAMP accumulation in PGD2-challenged human platelets (IC50 = 90 pM) and blocks PGD2-induced nasal congestion in a sheep allergic rhinitis model in vivo (by 99% at 0.1 mg/kg i.v.). MK-0524 decreases DP1-dependent basal cAMP level in HEK293 (1-100 nM) without affecting DP1-dependent basal ERK1/2 phosphorylation (up to 1 μM). | [storage]
Store at -20°C |
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