| Identification | Back Directory | [Name]
2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BENZIMIDAZOLE | [CAS]
312749-73-8 | [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
1H-Benzimidazole, 2-[[2-(4-chlorophenoxy)ethyl]thio]-
2-[2-(4-chlorophenoxy)ethylsulfanyl]-1H-benzimidazole
2-((2-(4-Chlorophenoxy)ethyl)thio)-1H-benzo[d]imidazole
2-[2-(4-Chloro-phenoxy)-ethylsulfanyl]-1H-benzoimidazole
LNCaP,Inhibitor,Androgen Receptor,CLP3094,inhibit,prostate,CLP 3094,resistance,CLP-3094,antiandrogens,cancer | [Molecular Formula]
C15H13ClN2OS | [MDL Number]
MFCD00805733 | [MOL File]
312749-73-8.mol | [Molecular Weight]
304.79 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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.
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| [References]
Susens et al. (2006), Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development, Neuropharmacology, 55 512
Lizarzaburu et al. (2012), Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus; Bioorg. Med. Chem. Lett., 22 5942
Murakoshi et al. (2017), Discovery and pharmacological effects of a novel GPR142 antagonist; Recept. Signal. Transduct. Res., 37 290 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
http://www.bocsci.com |
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