Setipiprant (ACT-129968) 是具有口服活性的、选择性的 CRTH2 拮抗剂。Setipiprant 与 hCRTH2 受体相互作用，IC₅₀ 为 6 nM。Setipiprant 抑制 prostanoid 受体 hDP₁ 以及 hEP₂，IC₅₀ 值分别为 1290 和 2600 nM。Setipiprant 可用于哮喘和鼻炎的研究。

Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC 50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP 1 and hEP 2 with IC 50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.

Solid

DP

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 h DP1, h EP2 and h EP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

1.19 Pharmacokinetic Properties of Setipiprant in Rats and Dogs.
AUC 0-last (ng?h/mL) CL (mL/min/kg)

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 36 mg/mL (89.46 mM)配制储备液