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A922500 (C007B-020267)

Catalog No.
C007B-020267
Mfr. No.
A408455-1ml
Mfr. Name
Aladdin Scientific
Qty/UOM
1
UOM
EA
Price: $428.99
List Price: $476.66

InformationA922500 A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.In vitroA 922500 inhibits the

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InformationA922500 A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.In vitroA 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1.In vivoZucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations.Cell Datacell lines:HUVECsConcentrations:Incubation Time:Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C26H24N2O4 Molecular Weight: 428.48
UPC:
51172323
Condition:
New
Availability:
2 weeks
Weight:
0.85 Ounces
HazmatClass:
No
WeightUOM:
LB
MPN:
A408455-1ml
CAS:
959122-11-3
Product Size:
1ml

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