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PZ0207

Sigma-Aldrich

PF-04620110

≥98% (HPLC)

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Synonym(s):
trans-4-[4-(4-Amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid
Empirical Formula (Hill Notation):
C21H24N4O4
CAS Number:
1109276-89-2
Molecular Weight:
396.44
UNSPSC Code:
12352200
PubChem Substance ID:
329823775
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL (clear solution)

storage temp.

room temp

SMILES string

Nc1ncnc2OCCN(C(=O)c12)c3ccc(cc3)[C@@H]4CC[C@H](CC4)CC(O)=O

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

Biochem/physiol Actions

PF-04620110 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that inhibits triacylglycerol synthesis in cells and in rodents.
PF-04620110 is known to regulate gut hormones. Inhibition of DGAT1 might serve as a good approach for the treatment of obesity and type 2 diabetes. DGAT1 inhibition might increase the oxidation of fatty acids, thus it is found to be protective against hepatic steatosis.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302

Precautionary Statements

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Specific role for acyl CoA: Diacylglycerol acyltransferase 1 (Dgat1) in hepatic steatosis due to exogenous fatty acids
Villanueva CJ, et al.
Hepatology, 50(2), 434-442 (2009)
Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
Cao J, et al.
The Journal of biological chemistry, jbc-M111 (2011)
Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
Cao J, et al.
The Journal of Biological Chemistry, jbc-M111 (2011)
New Therapeutic Strategies for Type 2 Diabetes: Small Molecule Approaches, 237-237 (2012)
Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
Cao J, et al.
Test, jbc-M111 (2011)
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