| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Tiphenazine (NN414), at least 100 times more powerful than diazoxide, hyperpolarizes βTC3 cell membranes and inhibits insulin release in βTC6, isolated rat islets, and human islets [2]. Tiphenazine and diazoxide had EC50 values in patch-clamp experiments of 0.45 and 31 µM, respectively. When applied at a concentration of 100 µM, tiphenazine activates Kir6.2/SUR1 channels, but not Kir6.2/SUR2A or Kir6.2/SUR2, which are expressed in both inside-out and whole-cell Xenopus laevis oocytes. expressed in recordings on big plaques [2]. Tiphenazine (IC50 = 0.15 µM) is a strong inhibitor of glucose-stimulated insulin release from βTC6 cells [1].
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|---|---|
| ln Vivo |
For three weeks, male VDF Zucker (fa/fa) rats given thiphenazine (NN414; 1.5 mg/kg; oral; twice daily) have reduced basal hyperglycemia and improved glucose tolerance. , and enhance in vitro insulin secretory response as well as lower hyperinsulinemia during the oral glucose tolerance test (OGTT) [1].
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| Animal Protocol |
Animal/Disease Models: Male Vancouver Diabetic Fat (VDF) Zucker rat [1]
Doses: 1.5 mg/kg Route of Administration: po (po (oral gavage)) twice a day; 3 weeks of treatment Experimental Results: Basal blood glucose diminished Dramatically, with an average decrease of 0.64 after 3 weeks of treatment mM. |
| References |
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| Additional Infomation |
Tifenazoxide is a thiadiazine derivative with hypoglycemic activity. Like sulfonylureas, tifenazoxide binds to ATP-sensitive inwardly-rectifier potassium Kir6.2/SUR1 (IKATP) channels on the membrane of pancreatic beta cells and stimulates insulin release to reduce blood glucose levels.
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| Molecular Formula |
C9H10CLN3O2S2
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|---|---|
| Molecular Weight |
291.77
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| Exact Mass |
290.99
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| CAS # |
279215-43-9
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| PubChem CID |
135410911
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| Appearance |
White to off-white solid powder
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| Vapour Pressure |
3.22E-08mmHg at 25°C
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| LogP |
3.059
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
469
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KYSFUHHFTIGRJN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H10ClN3O2S2/c1-9(2-3-9)12-8-11-5-4-6(10)16-7(5)17(14,15)13-8/h4H,2-3H2,1H3,(H2,11,12,13)
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| Chemical Name |
6-chloro-N-(1-methylcyclopropyl)-1,1-dioxo-4H-thieno[3,2-e][1,2,4]thiadiazin-3-imine
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| Synonyms |
NN-414; NN 414; Tifenazoxide
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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 : ~100 mg/mL (~342.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.57 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 (8.57 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 (8.57 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 | 3.4274 mL | 17.1368 mL | 34.2736 mL | |
| 5 mM | 0.6855 mL | 3.4274 mL | 6.8547 mL | |
| 10 mM | 0.3427 mL | 1.7137 mL | 3.4274 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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