312749-73-8
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
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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 |
| 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 |