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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
32 Results for "
CRTH2 receptor
" in MedChemExpress (MCE) Product Catalog:
Products (32)
32 Results for "CRTH2 receptor" in MCE Product Catalog:
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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 .
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4 Cited Publications
Synonyms: OC000459 sodium
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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 .
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1 Cited Publications
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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 .
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1 Cited Publications
Synonyms: DK-PGD2; 15-Oxo-13,14-dihydro-PGD2; 13,14-Dihydro-15-keto-PGD2
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13,14-Dihydro-15-keto prostaglandin D2 (DK-PGD2; 15-Oxo-13,14-dihydro-PGD2; 13,14-Dihydro-15-keto-PGD2) is a metabolite of Prostaglandin D2 (HY-101988) and acts as a CRTH2 agonist. 13,14-Dihydro-15-keto-prostaglandin D2 exhibits binding activity to CRTH2, induces cellular calcium signaling flux, and mediates eosinophilia in vivo. 13,14-Dihydro-15-keto-prostaglandin D2 activates the CRTH2 receptor, triggering Gi-dependent intracellular calcium mobilization and promoting the migration and recruitment of leukocytes from bone marrow to peripheral blood in vivo. 13,14-Dihydro-15-keto prostaglandin D2 is used in research on inflammation-related diseases, such as bronchial asthma .
Synonyms: AMG 853
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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 .
Cat. No.: HY-16635
CAS No.: 866460-33-5
Synonyms: ACT-129968; KYTH-105
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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 .
Synonyms: TM30089
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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 .
Synonyms: PGH2
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Prostaglandin H2 (PGH2) is an endothelium-derived contracting factor. Prostaglandin H2 can cause vasoconstriction. Prostaglandin H2 is the common precursor of all PGs and is produced by several cells that express cyclooxygen-ases. Prostaglandin H2 can activate PGD2 receptors CRTH2 and DP via interacting directly with the receptors and/or by giving rise to PGD2 after catalytic conversion by plasma proteins. Prostaglandin H2 can induce eosinophils migration and inhibit platelet aggregation. Prostaglandin H2 can accelerate the formation of dimers and higher oligomers of amyloid β1-42. Prostaglandin H2 can be used for the researches of inflammation and neurological disease, such as Alzheimer disease .
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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 .
Synonyms: 15(R)-15-Methyl PGD2
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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.
Synonyms: TM30089 Racemate
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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 .
Cat. No.: HY-118180
CAS No.: 916047-16-0
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CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM.
Cat. No.: HY-122558
CAS No.: 1263409-34-2
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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 .
Cat. No.: HY-135773
CAS No.: 312928-72-6
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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 .
Cat. No.: HY-116890
CAS No.: 916046-55-4
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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 .
Cat. No.: HY-U00423
CAS No.: 926661-54-3
Synonyms: Ramatroban analog
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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.
Cat. No.: HY-12284
CAS No.: 872365-16-7
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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 .
Cat. No.: HY-112604
CAS No.: 1416581-40-2
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MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
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(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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
