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PF-04620110

Item № 16425
CAS № 1109276-89-2
Purity ≥98%
product image
                (CAS 1109276-89-2)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     5 mg $74.00 0.00
     10 mg $126.00 0.00
     25 mg $296.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.

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

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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
A crystalline solid
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Shi, Y., and Burn, P. Lipid metabolic enzymes: Emerging drug targets for the treatment of obesity Nature Reviews.Drug Discovery 3, 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 Journal of Medicinal Chemistry 51, 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).

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