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Key Documents

PZ0207

Sigma-Aldrich

PF-04620110

≥98% (HPLC)

Synonym(s):

trans-4-[4-(4-Amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid

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About This Item

Empirical Formula (Hill Notation):
C21H24N4O4
CAS Number:
Molecular Weight:
396.44
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77

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Quality Level

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.[1] Inhibition of DGAT1 might serve as a good approach for the treatment of obesity and type 2 diabetes.[2] DGAT1 inhibition might increase the oxidation of fatty acids, thus it is found to be protective against hepatic steatosis.[3]

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Precautionary Statements

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

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.
Test, 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.
The Journal of Biological Chemistry, jbc-M111 (2011)

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