A potent, bioavailable inhibitor of DGAT-1
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PF-04620110

Item No. 16425

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-4-[4-(4-amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid
CAS Number
1109276-89-2
Molecular Formula
C21H24N4O4
Formula Weight
396.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
220, 244, 293 nm
SMILES
OC(C[C@@H]1CC[C@@H](C2=CC=C(N3CCOC(N=CN=C4N)=C4C3=O)C=C2)CC1)=O
InChi Code
InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
InChi Key
GEVVQZHMFVFGLN-HDJSIYSDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $102

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    10 mg

    $171

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    25 mg

    $396

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    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

    Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.

    OBESITY RESEARCH SOLUTIONS
    Product Description

    Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.1,2,3 PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.4 It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.4 PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shi, Y., and Burn, P. Lipid metabolic enzymes: Emerging drug targets for the treatment of obesity. Nat. Rev. Drug Discov. 3(8), 695-710 (2004).

    2. Zhao, G., Souers, A.J., Voorbach, M., et al. Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J. Med. Chem. 51(3), 380-383 (2008).

    3. Rudel, L.L., Lee, R.G., and Cockman, T.L. Acyl coenzyme A: Cholesterol acyltransferase types 1 and 2: Structure and function in atherosclerosis. Curr. Opin. Lipidol. 12(2), 121-127 (2001).

    4. Dow, R.L., Li, J.C., Pence, M.P., et al. Discovery of PF-04620110, a potent, selective, and orally bioavailable inhibitor of DGAT-1. ACS Med. Chem. Lett. 2(5), 407-412 (2011).