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Laropiprant

Chemical Structure : Laropiprant

CAS No.: 571170-77-9

Laropiprant (MK0524, MK-0524)

Catalog No.: PC-45826Not For Human Use, Lab Use Only.

Laropiprant (MK-0524) is a potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.

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Biological Activity

Laropiprant (MK-0524) is a potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.
Laropiprant shows weaker affinity for TP (Ki=2.95 nM), no significant activity on EP1, EP2, EP3, EP4, FP, and IP.
Laropiprant inhibits the accumulation of cAMP in washed platelets and in plateletrich plasma challenged with PGD with IC50 of 0.09 nM and 4 nM, respectively.
Laropiprant displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.

Physicochemical Properties

M.Wt 435.8963
Formula C21H19ClFNO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-

References

1. Sturino CF, et al. J Med Chem. 2007 Feb 22;50(4):794-806.

2. Cheng K, et al. Proc Natl Acad Sci U S A. 2006 Apr 25;103(17):6682-7.

3. Philip G, et al. J Allergy Clin Immunol. 2009 Nov;124(5):942-8.e1-9.

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