CLP-3094

Research use only, not for human use.

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.

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..

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)

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

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(-20℃)

With Ice Pack

≥ 2 years