Free shipping on all orders over $ 500

DGAT-1 inhibitor 2

Cat. No. M14291
DGAT-1 inhibitor 2 Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?
Quality Control & Documentation
Biological Activity

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents. IC50 value: Target: DGAT-1 Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes.

Chemical Information
Molecular Weight 420.5
CAS Number 942999-61-3
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Candida J Rebello, et al. Obesity medications in development

[2] Nathan D Roe, et al. The Role of Diacylglycerol Acyltransferase (DGAT) 1 and 2 in Cardiac Metabolism and Function

[3] Jianwei Yan, et al. Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety

[4] Daisuke Tomimoto, et al. Pharmacological characterization of [trans-5'-(4-amino-7,7-dimethyl-2-trifluoromethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)-2',3'-dihydrospiro(cyclohexane-1,1'-inden)-4-yl]acetic acid monobenzenesulfonate (JTT-553), a novel acyl CoA:diacylglycerol transfera䲧璵Ỵ璶㧀璴羹癦

[5] Eun-Young Kwak, et al. Preclinical pharmacokinetic characterization of 2-(4-(4-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)-1H-benzo[d]imidazol-2-yl)phenyl)cyclohexyl) acetic acid, a novel DGAT-1 inhibitor

Related DGAT Products
PF-07202954

PF-07202954 is an orally active, weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2.PF-07202954 reduces hepatic triglycerides in an obese rat model.
ION224

ION224 is an antisense compound that targets DGAT-2 for studies related to non-alcoholic steatohepatitis (NASH).
PF-07055341

PF-07055341 is a DGAT1/2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH).
Ervogastat

Ervogastat is a DGAT2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH).
Pradigastat

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.
  Catalog
Abmole Inhibitor Catalog




Keywords: DGAT-1 inhibitor 2 supplier, DGAT, inhibitors, activators

 
Get to Know Us
Customer Support
Resources
Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.