| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Dose-dependently, VU0071063 (1 nM~1 mM; HEK-293 cells) activates Kir6.2/SUR1. In mouse islets, VU0071063 (0~20 μM; isolated cells) suppresses beta cell excitability. VU0071063 (10 μM; 1 hour; isolated cells) suppresses the release of insulin in response to glucose [1]. The β-cell membrane potential is hyperpolarized by VU0071063 in a dose-dependent and reversible manner, which prevents glucose-stimulated Ca2+ entry and insulin production. Tolbutamide counteracted the effect of VU0071063 on β-cell membrane potential, but the inert analog 34MT had no effect on glucose-stimulated insulin secretion, indicating that Kir6.2/SUR1 is the mediating factor [1].
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|---|---|
| ln Vivo |
At 60 minutes, VU0071063 (50 mg/kg; i.p.; 4 hours) significantly raises blood sugar levels [1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (10-12 weeks old) [1]
Doses: 50 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intraperitoneal (ip) injection Experimental Results: resulted in a significant increase in blood glucose at 60 minutes. |
| References |
| Molecular Formula |
C18H22N4O2
|
|---|---|
| Molecular Weight |
326.4
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| Exact Mass |
326.174
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| CAS # |
333415-38-6
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| PubChem CID |
590142
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
507.8±42.0 °C at 760 mmHg
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| Flash Point |
260.9±27.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
3.23
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
508
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZFZAIHKQJBMYLO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N4O2/c1-18(2,3)13-8-6-12(7-9-13)10-22-11-19-15-14(22)16(23)21(5)17(24)20(15)4/h6-9,11H,10H2,1-5H3
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| Chemical Name |
7-[(4-tert-butylphenyl)methyl]-1,3-dimethylpurine-2,6-dione
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| Synonyms |
VU 0071063; VU-0071063; VU0071063
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~306.38 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.66 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0637 mL | 15.3186 mL | 30.6373 mL | |
| 5 mM | 0.6127 mL | 3.0637 mL | 6.1275 mL | |
| 10 mM | 0.3064 mL | 1.5319 mL | 3.0637 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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