A TGH/CES1 inhibitor
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GR148672X

Item No. 28756

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,4,4-trifluoro-1-(2-thienyl)-1,2,3-butanetrione, 2-[(3-methylphenyl)hydrazone]
CAS Number
263890-70-6
Molecular Formula
C15H11F3N2O2S
Formula Weight
340.3
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C(/C(C(C1=CC=CS1)=O)=N/NC2=CC(C)=CC=C2)C(F)(F)F
InChi Code
InChI=1S/C15H11F3N2O2S/c1-9-4-2-5-10(8-9)19-20-12(14(22)15(16,17)18)13(21)11-6-3-7-23-11/h2-8,19H,1H3/b20-12+
InChi Key
YNUQHMHMYSUKFL-UDWIEESQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $295

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    10 mg

    $479

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    Product Description

    GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).1,2 It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.1 GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Borg-Capra, C.S., Lehner, R.J., and Vance, D.E. Method of screening for triacyglycerol hydrolase inhibitors. WO 01/16358 A2, (2001).

    2. Wei, E., Ben Ali, Y., Lyon, J., et al. Loss of TGH/Ces3 in mice decreases blood lipids, improves glucose tolerance, and increases energy expenditure. Cell Metab. 11(3), 183-193 (2010).