| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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T863 (T-863; DGAT-1) is a novel and potent inhibitor of diacylglycerol O-acyltransferase 1 (DGAT1) with the potential to be used for the treatment of obesity.
| 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].
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|---|---|
| ln Vivo |
T863 (30 mg/kg; mice) improves insulin adiposity, reduces heart and serum lipids, and induces weight reduction [1].
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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. |
| References |
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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)
|
| 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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