CLP-3094 | GPR142 Antagonist
2-{[2-(4-Chlorophenoxy)ethyl]thio}-1H-benzimidazole
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $65.00 | ||
| 25 mg | $260.00 |
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
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
2-{[2-(4-Chlorophenoxy)ethyl]thio}-1H-benzimidazole
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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
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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