A diacylglycerol acyltransferase 2 inhibitor
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PF-06424439

Item No. 17680

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[(3R)-1-[2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone, monomethanesulfonate
CAS Number
1469284-79-4
Molecular Formula
C22H26ClN7O • CH3SO3H
Formula Weight
536.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleWater: Soluble
SMILES
O=C(N1CCCC1)[C@@H]2CCCN(C3=NC(N=C(C4(CC4)N5N=CC(Cl)=C5)N6)=C6C=C3)C2.OS(C)(=O)=O
InChi Code
InChI=1S/C22H26ClN7O.CH4O3S/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-28;1-5(2,3)4/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27);1H3,(H,2,3,4)/t15-;/m1./s1
InChi Key
ZSTFDNQQOJUJFL-XFULWGLBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

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    10 mg

    $167

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    25 mg

    $354

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    Product Description

    PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC50 = 14 nM).1 It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Futatsugi, K., Kung, D.W., Orr, S.T., et al. Discovery and optimization of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2). J. Med. Chem. 58(18), 7173-7185 (2015).

    Product Citations

    Rubio-Atonal, L.F., Chang, J., Jacquemyn, J., et al. Glutamate decreases oxidative stress and lipid droplet formation in astrocytes. J. Cell Sci. 138(19), jcs263983 (2025).

    von Krusenstiern, A.N., Robson, R.N., Qian, N., et al. Identification of essential sites of lipid peroxidation in ferroptosis. Nat. Chem. Biol. 19(6), 719-730 (2023).