CLP-3094 | GPR142 Antagonist

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:

  1. 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
  2. Lizarzaburu et al. (2012), Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus; Med. Chem. Lett., 22 5942
  3. Murakoshi et al. (2017), Discovery and pharmacological effects of a novel GPR142 antagonist; Recept. Signal. Transduct. Res., 37 290
Weight 0.1 mg
Dimensions 0.1 × 0.1 × 0.1 cm
Size:

5 mg, 25 mg

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CAS:
312749-73-8
Catalog Number:
10-3382
Activity:
GPR142 Antagonist
Chemical Names:

2-{[2-(4-Chlorophenoxy)ethyl]thio}-1H-benzimidazole

Molecular Weight:
304.79
Molecular Formula:
C15H13ClN2OS
Solubility:
Soluble in DMSO (up to 45 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

CLP-3094 | GPR142 Antagonist

$65.00$260.00

CAS:
312749-73-8
Catalog Number:
10-3382
Activity:
GPR142 Antagonist
Chemical Names:

2-{[2-(4-Chlorophenoxy)ethyl]thio}-1H-benzimidazole

Molecular Weight:
304.79
Molecular Formula:
C15H13ClN2OS
Solubility:
Soluble in DMSO (up to 45 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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