产品
编 号：F567133
分子式：C15H13ClN2OS
分子量：304.79
分子式：C15H13ClN2OS
分子量：304.79
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
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10mg
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询价
结构图
CAS No: 312749-73-8
产品详情
生物活性：
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
体内研究：
CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantlylowerseverityofarthritisscoresthanvehicletreatedmice.Animal Model:CAIA mouse model (FemaleDBA1/Jmice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)
Dosage:30, 100 mg/kg
Administration:I.p. daily from Day 0 to Day 11
Result:Dose-dependently reduced, by not much, the arth-ritis scores.
体外研究：
CLP-3094 inhibits both an increase of intracellular Ca2+ concentration ([Ca2+]i) induced by L-tryptophan using CHO-K1 cells expressing GPR142 in the aequorin assay, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. The IC50 of CLP-3094 is 0.2 μM against 200 μM L-tryptophanfor the mouse receptor and 2.3 μM against 1 mM L-tryptophan for the human receptor in the aequorin assay. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists.
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
体内研究：
CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantlylowerseverityofarthritisscoresthanvehicletreatedmice.Animal Model:CAIA mouse model (FemaleDBA1/Jmice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)
Dosage:30, 100 mg/kg
Administration:I.p. daily from Day 0 to Day 11
Result:Dose-dependently reduced, by not much, the arth-ritis scores.
体外研究：
CLP-3094 inhibits both an increase of intracellular Ca2+ concentration ([Ca2+]i) induced by L-tryptophan using CHO-K1 cells expressing GPR142 in the aequorin assay, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. The IC50 of CLP-3094 is 0.2 μM against 200 μM L-tryptophanfor the mouse receptor and 2.3 μM against 1 mM L-tryptophan for the human receptor in the aequorin assay. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists.
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