CLP-3094

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CLP-3094 是一种有效的雄激素受体 BF3（结合功能 3）抑制剂。 BF3-IN-1 抑制 AR 转录活性，IC50 为 4 μM。 CLP-3094 是一种选择性且有效的 GPR142 拮抗剂。

CLP-3094 is a potent androgen receptor BF3 (binding function 3) inhibitor. BF3-IN-1 inhibits AR transcriptional activity with IC50 of 4 μM. CLP-3094 is a selective and potent GPR142 antagonist.(In Vitro):In the aequorin assay, CLP-3094 inhibits both an increase of intracellular Ca2+ concentration ([Ca2+]) induced by L-tryptophan using CHO-K1 cells expressing GPR142, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. In the aequorin assay, CLP-3094 has an IC50 of 0.2 μM for 200 μM L-tryptophan at the mouse receptor and 2.3 μM at 1 mM L-tryptophan at the human receptor. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists.(In Vivo):I.p. administration of 30, 100 mg/kg CLP-3094 daily from Day 0 to Day 11 consistently displayed significantly lower severity of arthritis scores than vehicle-treated mice and reduced the arthritis scores dose-dependently, by not much..

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 (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 11Result:Dose-dependently reduced, by not much, the arth-ritis scores.

2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE

Endocrinology/Hormones

Androgen Receptor (AR)

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312749-73-8

304.8

C15H13ClN2OS

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (328.09 mM)

Clc(cc1)ccc1OCCSc1nc(cccc2)c2[nH]1

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(-20℃)

With Ice Pack

≥ 2 years