产品
编 号：F487665
分子式：C24H19FN2O3
分子量：402.42
分子式：C24H19FN2O3
分子量：402.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 866460-33-5
产品详情
生物活性：
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.
体内研究：
1.19Pharmacokinetic Properties of Setipiprant in Rats and Dogs. AUC0-last (ng?h/mL)CL (mL/min/kg) T1/2 (hr) F (%)
RatsIV 2 mg/kg585001.3644
DogsPO 10 mg/kg9110055
体外研究：
Setipiprant (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.
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.
体内研究：
1.19Pharmacokinetic Properties of Setipiprant in Rats and Dogs. AUC0-last (ng?h/mL)CL (mL/min/kg) T1/2 (hr) F (%)
RatsIV 2 mg/kg585001.3644
DogsPO 10 mg/kg9110055
体外研究：
Setipiprant (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.
产品资料
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