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CRTh2 (DP2) receptor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14973
    Vidupiprant

    AMG 853

    		 Prostaglandin Receptor Inflammation/Immunology
    Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment .
    Vidupiprant
  • HY-15342
    Timapiprant
    4 Publications Verification

    OC000459

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils .
    Timapiprant
  • HY-15342A
    Timapiprant sodium
    4 Publications Verification

    OC000459 sodium

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils .
    Timapiprant sodium
  • HY-114141
    BI-671800

    		Prostaglandin Receptor Inflammation/Immunology Endocrinology
    BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively . BI-671800 has potential for the treatment of poorly controlled asthma .
    BI-671800
  • HY-125782
    15(R)​-​15-​Methyl prostaglandin D2

    15(R)-15-Methyl PGD2

    		 Prostaglandin Receptor Metabolic Disease
    15(R)-15-Methyl prostaglandin D2 (15(R)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1and CRTH2/DP2. 15(R)-15-Methyl prostaglandin D2 is a potent, selective agonist for the CRTH2/DP2 receptor. The EC50 values for eosinophil CD11b expression, actin polymerization, and chemotaxis are 1.4, 3.8, and 1.7 nM, respectively, each of which is approximately 3-5 fold lower than those for PGD2. In contrast the EC50 for the DP1-mediated increase in platelet cAMP by 15(R)-15-methyl PGD2 is >10 μM.
    15(R)​-​15-​Methyl prostaglandin D2
  • HY-118180
    CAY10595

    		Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM.
    CAY10595
  • HY-122558
    AM432 sodium

    		Prostaglandin Receptor Neurological Disease
    AM432 (sodium) is a potent and selective antagonist of the DP2 receptor (CRTH2). AM432 (sodium) exhibits excellent potency in a human whole blood eosinophil shape change assay with prolonged incubation. AM432 (sodium) also demonstrates excellent pharmacokinetics in dog and mouse models of inflammatory disease .
    AM432 sodium
  • HY-U00423
    CRTH2-IN-1

    Ramatroban analog

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.
    CRTH2-IN-1
  • HY-116890
    CRTh2 antagonist 4

    		Prostaglandin Receptor Inflammation/Immunology
    CRTh2 antagonist 4 (compound 58) is an inhibitor (IC50: 212 nM) of TH2 lymphocyte (CRTH2 or DP2) receptor with high binding affinity (Ki= 37 nM). CRTh2 antagonist 4 can be used in the study of severe allergic diseases .
    CRTh2 antagonist 4
  • HY-126911
    11-keto Fluprostenol

    Fluprostenol Prostaglandin D2

    		 Prostaglandin Receptor Endocrinology
    11-keto Fluprostenol is an analog of prostaglandin D2 (PGD2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-11 of fluprostenol yields 11-keto fluprostenol. 11-keto Fluprostenol exhibits moderate binding to the CRTH2/DP2 receptor compared to PGD2 and essentially no activity at the DP1 receptor.
    11-keto Fluprostenol
  • HY-116811
    AZ-11665362

    		Prostaglandin Receptor Serotonin Transporter Aldose Reductase Cytochrome P450 Inflammation/Immunology
    AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC50 of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases .
    AZ-11665362

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