| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vivo |
BMS-820132 (Compound 31) (3 μmol/kg, 30 μmol/kg; minimum; single dose) reduces contact levels of high-fat diet-induced body weight (DIO) electrodes in the baseline tolerance test (OGTT) [1] BMS -820132 (10-200 mg/kg; lateral; once daily for 1 month) resulted in normal weight recovery but had no effect on ZDF development, suggesting that BMS-820132 toxicity is secondary to the potent GK BMS-820132 ( 10 mg/kg-120 mg/kg; lateral; once daily for 1 month) had no significant effect on food consumption in dogs [2]. Pharmacokinetic analysis in animal models [1] Route Dose (mg/kg) Cmax (μM) Tmax (h) AUC0-24 h (μM·h) T1/2 (h) CLTp (mL/min/kg ) Vss (L /kg) F (L/kg) Mouse iv 2.5 24.9 2.1 2.9 0.3 po 5 14.1 0.5 49.7 100 Rat iv 2.5 16.6 0.9 4.4 0.3 po 5 13.0 0.9 29.5 90 Dog iv 3 12.3 1.8 7.2 0 .5 po 3 4.9 0.8 8.0 66 Monkey IV 3 3.8 1.9 22.7 1.1 po 3 3.8 1.3 0.57 15
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| Animal Protocol |
Animal/Disease Models: Zucker diabetic obese (ZDF) rat and normal SD rat [2]
Doses: 10 mg/kg, 50 mg/kg, 200 mg /kg Route of Administration: PO; one time/day for 1 month Experimental Results: Starting from day 7, body weight gain was diminished in SD rats (11% lower than controls), but not in ZDF rats. Animal/Disease Models: Beagle [2] Doses: 10 mg/kg, 60 mg/kg, 120 mg/kg Route of Administration: PO; one time/day for 1 month Experimental Results: There was no significant difference in food consumption in the dog model . |
| References |
| Molecular Formula |
C26H33N6O7P
|
|---|---|
| Molecular Weight |
572.549986600876
|
| Exact Mass |
572.214
|
| CAS # |
1001419-18-6
|
| PubChem CID |
58265877
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
13
|
| Heavy Atom Count |
40
|
| Complexity |
884
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
P(CN1C=CC(NC(C2C=C(C=C(C=2)OC2=CN=C(C=N2)C(N2CCC2)=O)OC(C)C)=O)=N1)(=O)(OCC)OCC
|
| InChi Key |
OYUDYQMFVRHPIY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H33N6O7P/c1-5-36-40(35,37-6-2)17-32-11-8-23(30-32)29-25(33)19-12-20(38-18(3)4)14-21(13-19)39-24-16-27-22(15-28-24)26(34)31-9-7-10-31/h8,11-16,18H,5-7,9-10,17H2,1-4H3,(H,29,30,33)
|
| Chemical Name |
3-[5-(azetidine-1-carbonyl)pyrazin-2-yl]oxy-N-[1-(diethoxyphosphorylmethyl)pyrazol-3-yl]-5-propan-2-yloxybenzamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~43.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.37 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 | 1.7466 mL | 8.7329 mL | 17.4657 mL | |
| 5 mM | 0.3493 mL | 1.7466 mL | 3.4931 mL | |
| 10 mM | 0.1747 mL | 0.8733 mL | 1.7466 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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