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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
41 Results for "
CRTh2
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "CRTh2" in MCE Product Catalog:
4
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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 .
4
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 .
2
2 Cited Publications
Cat. No.: HY-15950
CAS No.: 802904-66-1
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AZD1981 is the antagonist for GPR44 (also known also PTGDR2, DP2 or CRTh). AZD1981 blocks the binding of PGD2 to CRTH2. AZD1981 exhibits immunomodulatory effects and can be used in research of chronic spontaneous urticaria [2].
1
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 .
1
1 Cited Publications
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MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
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-B0745
CAS No.: 116649-85-5
Synonyms: BAY u3405
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Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
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 [2] .
Cat. No.: HY-112265
CAS No.: 1379445-54-1
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CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM.
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 [2] .
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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 [2].
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CRTh2 antagonist 2 is selective and potent CRTH2 antagonist extracted from patent US20140148470A1, compound Example 1, has an IC50 of ≤10 nM. CRTh2 antagonist 2 can be used in research of androgenic alopecia .
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 [2].
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 .
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.
Cat. No.: HY-123596
CAS No.: 1420071-13-1
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LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC50 of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma .
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-124065
CAS No.: 1202891-16-4
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ARRY-502 is an orally active, potent and selective CRTh2 antagonist. ARRY-502 blocks PGD2-mediated Th2 inflammation (e.g., eosinophil activation, airway hyperresponsiveness). ARRY-502 is promising for research of Th2-related asthma .
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.
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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
