A hepatoselective glucokinase activator
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PF-04991532

Item No. 17683

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[[(2S)-3-cyclopentyl-1-oxo-2-[4-(trifluoromethyl)-1H-imidazol-1-yl]propyl]amino]-3-pyridinecarboxylic acid
CAS Number
1215197-37-7
Molecular Formula
C18H19F3N4O3
Formula Weight
396.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C([C@@H](N1C=C(C(F)(F)F)N=C1)CC2CCCC2)NC3=CC=C(C(O)=O)C=N3
InChi Code
InChI=1S/C18H19F3N4O3/c19-18(20,21)14-9-25(10-23-14)13(7-11-3-1-2-4-11)16(26)24-15-6-5-12(8-22-15)17(27)28/h5-6,8-11,13H,1-4,7H2,(H,27,28)(H,22,24,26)/t13-/m0/s1
InChi Key
GKMLFBRLRVQVJO-ZDUSSCGKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $124

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    25 mg

    $293

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    50 mg

    $553

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    PF-04991532 is a hepatoselective glucokinase activator (EC50 = 90 nM in a cell-free assay using the recombinant human enzyme).1 It increases 2-deoxyglucose uptake and decreases glucose production in isolated rat hepatocytes (EC50s = 1.261 and 0.626 µM, respectively).2 PF-04991532 reduces fasting and postprandial plasma glucose levels in rat models of type 2 diabetes.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pfefferkorn, J.A., Guzman-Perez, A., Litchfield, J., et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. 55(3), 1318-1333 (2012).

    2. Erion, D.M., Lapworth, A., Amor, P.A., et al. The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats. PLoS One 9(5), 1-9 (2014).