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312749-73-8

312749-73-8 structure
312749-73-8 structure
  • Name: 2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE
  • Chemical Name: 2-{[2-(4-Chlorophenoxy)ethyl]sulfanyl}-1H-benzimidazole
  • CAS Number: 312749-73-8
  • Molecular Formula: C15H13ClN2OS
  • Molecular Weight: 304.794
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2021-09-10 18:47:52
  • Modify Date: 2024-01-10 13:28:32
  • 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)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].
Name 2-{[2-(4-Chlorophenoxy)ethyl]sulfanyl}-1H-benzimidazole
Synonyms 2-(1H-benzimidazol-2-ylsulfanyl)ethyl 4-chlorophenyl ether
MFCD00805733
1H-Benzimidazole, 2-[[2-(4-chlorophenoxy)ethyl]thio]-
2-{[2-(4-Chlorophenoxy)ethyl]sulfanyl}-1H-benzimidazole
Description 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)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].
Related Catalog
In Vitro 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[2].
In Vivo CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantly lower severity of arthritis scores than vehicletreated mice[2]. Animal Model: CAIA mouse model (Female DBA1/J mice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)[2] 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.
References

[1]. Munuganti RS, et al. Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives. J Med Chem. 2013;56(3):1136-1148.

[2]. Murakoshi M, et al. Discovery and pharmacological effects of a novel GPR142 antagonist. J Recept Signal Transduct Res. 2017;37(3):290-296.
Density 1.4±0.1 g/cm3
Boiling Point 509.6±56.0 °C at 760 mmHg
Molecular Formula C15H13ClN2OS
Molecular Weight 304.794
Flash Point 262.0±31.8 °C
Exact Mass 304.043701
LogP 5.08
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.693

Chemsrc provides CAS#:312749-73-8 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 312749-73-8 | Chemsrc address: https://m.chemsrc.com/en/baike/1605753.html

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