SetipiprantSetipiprant
MedChemExpress (MCE)
HY-16635
866460-33-5
ACT-129968
KYTH-105
98.23%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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 (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[1]. 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[1]. Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and >10000 nM, respectively[1].
1.19 Pharmacokinetic Properties of Setipiprant in Rats and Dogs[1]. AUC0-last (ng•h/mL) CL (mL/min/kg) T1/2 (hr) F (%) RatsIV 2 mg/kg 58500 1.3 6 44 DogsPO 10 mg/kg 91100 55
hCRTH2 6 nM (IC50) hDP1 1290 nM (IC50) EP2 2600 nM (IC50)
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[1]. Heinz Fretz, et al. Identification of 2 (2-(1-Naphthoyl)-8-fluoro-3,4-dihydro 1H pyrido[4,3 b]indol-5(2H) yl)acetic Acid (Setipiprant/ACT 129968), a Potent, Selective, and Orally Bioavailable Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTH2) Antagonis. 2013.