| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
T863 targets DGAT1, the enzyme that catalyzes the final step of triacylglycerol synthesis. It has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2.
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|---|---|
| ln Vitro |
T863 increases insulin-stimulated insulin content for three days, indicating that adipocytes may raise insulin readings following DGAT1 inhibition in 3T3-L1 adipocyte secretion [1].
In vitro, T863 inhibits DGAT1 with an IC50 of 15 nM. It effectively inhibits triacylglycerol synthesis in cells by interacting with the acyl-CoA binding site of DGAT1. |
| ln Vivo |
T863 (30 mg/kg; mice) improves insulin adiposity, reduces heart and serum lipids, and induces weight reduction [1].
In vivo, T863 (20 mg/kg) reduces plasma triacylglycerol levels, the ratio of triacylglycerols to diacylglycerols, and body weight in a mouse model of diet-induced obesity. It has potential for the treatment of obesity. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for T863 typically involve evaluating its inhibitory activity against purified DGAT1 enzyme using radiometric or chromatographic assays. IC50 values are determined by measuring the incorporation of labeled acyl-CoA into triacylglycerol.
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| Cell Assay |
For in vitro cell-based assays, T863 is dissolved in DMSO and applied to cultured cells such as hepatocytes or adipocytes at concentrations ranging from 1 nM to 10 µM. Effects on triacylglycerol synthesis, lipid accumulation, and cell viability are assessed after 24-72 hours of treatment.
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| Animal Protocol |
Animal/Disease Models: C57BL6 normal mice (8 weeks old) or diet-induced obese (DIO) mice (10 months old, fed high-fat diet for 8 months) [1]
Doses: 30 mg/kg (5 μL/g) Route of Administration: po (po (oral gavage)) one time/day on days 1-7, twice a day on days 8-14. Experimental Results: Dramatically delayed fat absorption, leading to lipid accumulation in the distal small intestine of mice, simulating the effect of DGAT1 gene elimination. In vivo animal studies commonly use diet-induced obesity mouse models. T863 is administered orally at doses ranging from 1-100 mg/kg. Efficacy is evaluated by measuring plasma lipids, body weight, adipose tissue mass, and histopathological examination of liver and adipose tissues. |
| ADME/Pharmacokinetics |
T863 is orally active. It has a molecular formula of C22H26N4O3 and a molecular weight of 394.47 g/mol. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
T863 has a favorable safety profile with no significant toxicity reported at research doses. Its selectivity for DGAT1 over other acyltransferases minimizes off-target effects.
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| References |
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| Additional Infomation |
T863 is a valuable tool compound for studying the role of DGAT1 in lipid metabolism and obesity. It has potential therapeutic applications in the treatment of obesity and metabolic syndrome.
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| Molecular Formula |
C22H26N4O3
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|---|---|
| Molecular Weight |
394.46684
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| Exact Mass |
394.2
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| CAS # |
701232-20-4
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| PubChem CID |
9865421
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
616.6±55.0 °C at 760 mmHg
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| Flash Point |
326.7±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.674
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| LogP |
3.06
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FUIYMYNYUHVDPT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)
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| Chemical Name |
2-[4-[4-(4-amino-7,7-dimethylpyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]cyclohexyl]acetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~126.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL | |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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