Setipiprant

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^[1]. IC50 & Target: IC50: 6 nM (hCRTH2), 1290 nM (hDP₁), 2600 nM (hEP₂)^[1] 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^[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]. In Vivo: Pharmacokinetic Properties of Setipiprant in Rats and Dogs^[1].

	AUC0-last (ng?h/mL)	CL (mL/min/kg)	T1/2 (hr)	F (%)
Rats IV 2 mg/kg	58500	1.3	6	44
Dogs PO 10 mg/kg	91100			55