Laropiprant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性前列腺素 D2 (PGD2) 受体 (DP1) 拮抗剂，Ki 为 0.57 nM。

A potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM; shows weaker affinity for TP (Ki=2.95 nM), no significant activity on EP1, EP2, EP3, EP4, FP, and IP; 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; displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.Dyslipidemia Withdrawn.

Laropiprant (0.01-1000 μM; 10 mins; HEK293 cells) is an inverse agonist of DP1 cAMP signaling and reduces DP1 cAMP signaling below basal levels.Laropiprant (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression.

Laropiprant (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles.Pharmacokinetic Analysis in Male Sprague-Dawley rats.

MK 0524 | MK-0524

GPCR/G Protein

Prostaglandin Receptor

Prostaglandin Receptor

Cardiovascular Disease

Dyslipidemia

571170-77-9

435.8963

C21H19ClFNO4S

>98% (HPLC)

10 mM in DMSO

O=C(O)C[C@H]1CCC2=C1N(CC3=CC=C(Cl)C=C3)C4=C2C=C(F)C=C4S(=O)(C)=O

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

(-20℃)

With Ice Pack

≥ 2 years