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T863

Cat. No. M8388
T863 Structure
Synonym:

DGAT-1 inhibitor

Size Price Availability Quantity
5mg USD 92  USD92 In stock
10mg USD 138  USD138 In stock
25mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

Chemical Information
Molecular Weight 394.47
Formula C22H26N4O3
CAS Number 701232-20-4
Form Solid
Solubility (25°C) DMSO: 15 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] Stanzin Dawa, et al. Inhibition of Granuloma Triglyceride Synthesis Imparts Control of Mycobacterium tuberculosis Through Curtailed Inflammatory Responses

[2] Maya W Haaker, et al. Identification of potential drugs for treatment of hepatic lipidosis in cats using an in vitro feline liver organoid system

[3] Sabrina J Nolan, et al. Novel Approaches To Kill Toxoplasma gondii by Exploiting the Uncontrolled Uptake of Unsaturated Fatty Acids and Vulnerability to Lipid Storage Inhibition of the Parasite

[4] Minal Mulye, et al. Altering lipid droplet homeostasis affects Coxiella burnetii intracellular growth

[5] Jingsong Cao, et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases

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Keywords: T863, DGAT-1 inhibitor supplier, DGAT, inhibitors, activators

 
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