An agonist of GPR119
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GSK1292263

Item No. 26181

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[1-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methoxy]-2-[4-(methylsulfonyl)phenyl]-pyridine
CAS Number
1032823-75-8
Molecular Formula
C23H28N4O4S
Formula Weight
456.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/mL
λmax
224, 276, 296 nm
SMILES
CS(C1=CC=C(C2=CC=C(OCC3CCN(C4=NC(C(C)C)=NO4)CC3)C=N2)C=C1)(=O)=O
InChi Code
InChI=1S/C23H28N4O4S/c1-16(2)22-25-23(31-26-22)27-12-10-17(11-13-27)15-30-19-6-9-21(24-14-19)18-4-7-20(8-5-18)32(3,28)29/h4-9,14,16-17H,10-13,15H2,1-3H3
InChi Key
AYJRTVVIBJSSKN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $131

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    10 mg

    $236

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    25 mg

    $552

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    50 mg

    $895

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    Product Description

    GSK1292263 is an agonist of G protein-coupled receptor 119 (GPR119; EC50 = 43.9 nM in CHO-K1 cells expressing human receptors).1 It inhibits increases in sterol regulatory element binding protein-1 (SREBP-1) levels induced by the LXR agonist T0901317 and increases activation of AMPK in HepG2 cells in a concentration-dependent manner.2 GSK1292263 also inhibits breast cancer resistant protein (BCRP) and organic anion transporting polypeptide 1B1 (OATP1B1) by 52 and 40%, respectively, when used at a concentration of 3 μM.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Park, Y.H., Choi, H.H., Lee, D.H., et al. YH18421, a novel GPR119 agonist exerts sustained glucose lowering and weight loss in diabetic mouse model. Arch. Pharm. Res. 40(6), 772-782 (2017).

    2. Yang, J.W., Kim, H.S., Im, J.H., et al. GPR119: A promising target for nonalcoholic fatty liver disease. FASEB J. 30(1), 324-335 (2016).

    3. Polli, J.W., Hussey, E., Bush, M., et al. Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: From in vitro data to clinical study design. Xenobiotica 43(6), (2013).