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Laropiprant

CAS No. 571170-77-9

Laropiprant( MK 0524 | MK-0524 )

Catalog No. M15081 CAS No. 571170-77-9

A potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Laropiprant
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.
  • Description
    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displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.Dyslipidemia Withdrawn.
  • In Vitro
    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.
  • In Vivo
    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.
  • Synonyms
    MK 0524 | MK-0524
  • Pathway
    GPCR/G Protein
  • Target
    Prostaglandin Receptor
  • Recptor
    Prostaglandin Receptor
  • Research Area
    Cardiovascular Disease
  • Indication
    Dyslipidemia

Chemical Information

  • CAS Number
    571170-77-9
  • Formula Weight
    435.8963
  • Molecular Formula
    C21H19ClFNO4S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(O)C[C@H]1CCC2=C1N(CC3=CC=C(Cl)C=C3)C4=C2C=C(F)C=C4S(=O)(C)=O
  • Chemical Name
    Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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