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Setipiprant
CAS No. 866460-33-5
Setipiprant( ACT-129968 | ACT 129968 | KYTH 105 | Setipiprant )
Catalog No. M19195 CAS No. 866460-33-5
Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 23 | In Stock |
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| 10MG | 35 | In Stock |
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| 25MG | 65 | In Stock |
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| 50MG | 106 | In Stock |
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| 100MG | 170 | In Stock |
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| 200MG | 250 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameSetipiprant
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NoteResearch use only, not for human use.
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Brief DescriptionSetipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2).
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DescriptionSetipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells.(In Vitro):Setipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence of Human Serum Albumin (HSA) in the assay buffer with IC50 values of 6 and 340 nM, respectively.Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC50 values of 30, 80 and 235 nM, respectively.Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively.(In Vivo):Pharmacokinetic Properties of Setipiprant in Rats and Dogs.
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In VitroSetipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence ofHuman Serum Albumin (HSA) in the assay buffer with IC50 values of 6 and 340 nM, respectively.Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC50 values of 30, 80 and 235 nM, respectively.Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively.
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In Vivo——
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SynonymsACT-129968 | ACT 129968 | KYTH 105 | Setipiprant
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PathwayOthers
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TargetOther Targets
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RecptorCRTh2
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Research AreaInflammation/Immunology
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Indication——
Chemical Information
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CAS Number866460-33-5
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Formula Weight402.42
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Molecular FormulaC24H19FN2O3
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 36 mg/mL; 89.46 mM
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SMILESC1CN(CC2=C1N(C3=C2C=C(C=C3)F)CC(=O)O)C(=O)C4=CC=CC5=CC=CC=C54
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Chemical Name2-(2-(1-naphthoyl)-8-fluoro-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl)acetic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Diamant Z., et al. Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52.
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