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Home - Products - GPCR/G Protein - Prostaglandin Receptor - Laropiprant

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
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 83 In Stock
5MG 75 In Stock
10MG 109 In Stock
25MG 219 In Stock
50MG 330 In Stock
100MG 472 In Stock
200MG 644 In Stock
500MG Get Quote In Stock
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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displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.Dyslipidemia Withdrawn.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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