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CRTH2 receptor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111271
    L 888607
    1 Publications Verification

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
    L 888607
  • HY-111271B
    (R)-L 888607

    		Prostaglandin Receptor Drug Isomer Inflammation/Immunology Endocrinology
    (R)-L 888607 is the isomer of L 888607 (HY-111271), and can be used as an experimental control. L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
    (R)-L 888607
  • HY-13706
    CAY10471 Racemate

    TM30089 Racemate

    		 Prostaglandin Receptor Endocrinology Cancer
    CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2 .
    CAY10471 Racemate
  • HY-19499
    AMG-009

    		Prostaglandin Receptor Inflammation/Immunology Endocrinology
    AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.
    AMG-009
  • HY-135773
    CRTh2 antagonist 3

    		Prostaglandin Receptor PDK-1 Cardiovascular Disease Inflammation/Immunology
    CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist . CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation .
    CRTh2 antagonist 3
  • 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-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-12284
    NVP-QAV680

    		Prostaglandin Receptor Inflammation/Immunology
    NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
    NVP-QAV680
  • 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-112604
    MK-8318

    		Prostaglandin Receptor Inflammation/Immunology Endocrinology
    MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
    MK-8318
  • 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-13706A
    CAY10471

    TM30089

    		 Prostaglandin Receptor Inflammation/Immunology
    CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model .
    CAY10471
  • HY-16635
    Setipiprant

    ACT-129968; KYTH-105

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis .
    Setipiprant
  • HY-114623
    Prostaglandin D2 methyl ester

    		Prostaglandin Receptor Endocrinology
    Prostaglandin D2 methyl ester is a prodrug form of Prostaglandin D2. Prostaglandin D2 methyl ester binds to the human and mouse PGD2 receptors (DP and CRTH2) with Ki values of 160 nM, 175 nM, 460 nM, and 270 nM for mCRTH2, mDP, hCRTH2, and hDP, respectively .
    Prostaglandin D2 methyl ester
  • 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-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-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-15342
    Timapiprant
    3 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
    3 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