An agonist of GPR119
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APD597

Item No. 22950

Technical Information
Formal Name
4-[[5-methoxy-6-[[2-methyl-6-(methylsulfonyl)-3-pyridinyl]amino]-4-pyrimidinyl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester
CAS Number
897732-93-3
Synonyms
  • JNJ-38431055
Molecular Formula
C21H29N5O6S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 25mg/mLDMSO: 25mg/mLEthanol: 50mg/mLEthanol:PBS (pH 7.2) (1:3): 0.25mg/mL
λmax
311 nm
SMILES
CC(OC(N1CCC(OC2=C(OC)C(NC3=C(C)N=C(S(C)(=O)=O)C=C3)=NC=N2)CC1)=O)C
InChi Code
InChI=1S/C21H29N5O6S/c1-13(2)31-21(27)26-10-8-15(9-11-26)32-20-18(30-4)19(22-12-23-20)25-16-6-7-17(24-14(16)3)33(5,28)29/h6-7,12-13,15H,8-11H2,1-5H3,(H,22,23,25)
InChi Key
WPDCHTSXOPUOII-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    APD597 is an orally bioavailable agonist of GPR119 that has EC50 values of 46 and 421 nM for the human and rat receptors, respectively, in a homologous time-resolved fluorescence (HTRF) assay.1 It increases insulin secretion stimulated by a high, but not low, concentration of glucose in isolated mouse pancreatic β-cells and in isolated human islets.2 APD597 (20 mg/kg) increases levels of glucagon-like peptide-1 (GLP-1; Item No. 24460) induced by glucose in mice. It also decreases blood glucose levels in an oral glucose tolerance test in mice when administered at doses of 1 and 10 mg/kg and in Zucker diabetic rats at a dose of 3 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Semple, G., Lehmann, J., Wong, A., et alDiscovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile. Bioorg. Med. Chem. Lett. 22(4), 1750-1755 (2012).

    2. Huan, Y., Jiang, Q., Li, G., et alThe dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci. Rep. 7(1), 4351 (2017).