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252801

Sigma-Aldrich

DGAT-1 Inhibitor, A 922500

The DGAT-1 Inhibitor, A 922500, also referenced under CAS 959122-11-3, controls the biological activity of DGAT-1. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

Synonym(s):

DGAT-1 Inhibitor, A 922500

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About This Item

Empirical Formula (Hill Notation):
C26H24N2O4
CAS Number:
Molecular Weight:
428.48
UNSPSC Code:
12352200

Quality Level

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

light yellow

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1

InChI key

BOZRFEQDOFSZBV-DHIUTWEWSA-N

General description

An orally, bioavailable human and mouse diacylglycerol acyltransferase DGAT-1 inhibitor (IC50 = 9nM and 22 nM, respectively), which may target DGAT-2 (IC50 = 53 µM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50 = 296 µM) with equal or less potencies. In vivo activities indicate an effective reduction in serum triglycerides, FFA concentrations, and total cholesterol by 53%, 55% and 25%, respectively, compared to baseline, when administered orally at 3 mg/kg daily dosages in Dyslipidemic Hamsters. Similar reductions in triglyceride and FFA concentrations were shown in Zucker fatty rats.
An orally, bioavailable human and mouse diacylglycerol acyltransferase DGAT-1 inhibitor (IC50 = 9nM and 22 nM, respectively), which may target DGAT-2 (IC50 = 53 uM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50 = 296 uM) with equal or less potencies. In vivo activities indicate an effective reduction in serum triglycerides, FFA concentrations, and total cholesterol by 53%, 55% and 25%, respectively, compared to baseline, when administered orally at 3 mg/kg daily dosages in Dyslipidemic Hamsters. Similar reductions in triglyceride and FFA concentrations were shown in Zucker fatty rats.

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

King, A.J., et al. 2009. J. Pharmacol. Exp. Ther.330, 526.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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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