2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE
- Product Name
- 2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE
- CAS No.
- 312749-73-8
- Chemical Name
- 2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE
- Synonyms
- CLP-3094;EU-0033941;ZINC02074828;BAS 00450541;AH-034/34344061;CLP-3094, 10 mM in DMSO;2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE;2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE;2-[2-(4-chlorophenoxy)ethylsulfanyl]-1H-benzimidazole;1H-Benzimidazole, 2-[[2-(4-chlorophenoxy)ethyl]thio]-
- CBNumber
- CB4417228
- Molecular Formula
- C15H13ClN2OS
- Formula Weight
- 304.79
- MOL File
- Mol file
2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE Property
- storage temp.
- RT
- solubility
- Soluble in DMSO (up to 45 mg/ml)
- form
- solid
- color
- Off-white
- Stability:
- Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Safety
- HazardClass
- IRRITANT
N-Bromosuccinimide Price
- Product number
- 066588
- Product name
- 2-{[2-(4-Chlorophenoxy)ethyl]thio}-1H-benzimidazole
- Packaging
- 500mg
- Price
- $119
- Updated
- 2021/12/16
- Product number
- CD11147489
- Product name
- 2-((2-(4-Chlorophenoxy)ethyl)thio)-1H-benzo[d]imidazole
- Purity
- 97%
- Packaging
- 1g
- Price
- $872
- Updated
- 2021/12/16
2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE Chemical Properties,Usage,Production
Description
GPR142 is highly expressed in the pancreas and immune system and shares 33% homology with GPR139.1 Endogenous agonists identified to date include aromatic amino acids such as tryptophan and phenylalanine.2?CLP-3094? (312749-73-8) was identified as a potent and selective GPR142 antagonist with an IC50=2.3 μM against 1 mM L-tryptophan. It inhibited insulin secretion from islets induced by L-tryptophan and other agonists and displayed anti-inflammatory activity in a mouse arthritis model.3
Uses
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].
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] UTE SÜSENS. Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development[J]. Neuropharmacology, 2006, 50 4: Pages 512-520. DOI:10.1016/j.neuropharm.2005.11.003
[2] MIKE LIZARZABURU . Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus[J]. Bioorganic & Medicinal Chemistry Letters, 2012, 22 18: Pages 5942-5947. DOI:10.1016/j.bmcl.2012.07.063
[3] MICHIKO MURAKOSHI. Discovery and pharmacological effects of a novel GPR142 antagonist[J]. Journal of Receptors and Signal Transduction, 2017, 87 1: 290-296. DOI:10.1080/10799893.2016.1247861
2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE Preparation Products And Raw materials
Raw materials
Preparation Products
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