A potent GPR39 agonist
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GPR39-C3

Item No. 25445

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]-methanesulfonamide
CAS Number
1621175-65-2
Molecular Formula
C18H19ClN6O2S
Formula Weight
418.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml
λmax
229, 331 nm
SMILES
CS(NC1=CC=C(CNC2=NC(NC)=NC(C3=CC=CC=N3)=C2)C(Cl)=C1)(=O)=O
InChi Code
InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24)
InChi Key
DRSZMILOMUPIBJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.1 It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Peukert, S., Hughes, R., Nunez, J., et al. Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med. Chem. Lett. 5(10), 1114-1118 (2014).