Size | Price | Stock | Qty |
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100mg |
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500mg |
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Other Sizes |
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ln Vitro |
Mitiglinide calcium hydrate does not significantly inhibit Kir6.2/SUR2A or Kir6.2/, even at high doses. However, it does inhibit Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM). SUR2B channel current (less than 10 μM in a greater number of COS-1 cells) [1].
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ln Vivo |
The increase in plasma glucose levels following a meal and the rise in the area under the curve of plasma glucose levels (AUC glucose) within five hours following a meal are both inhibited by mitiglide calcium hydrate (1-3 mg/kg; oral) [2].
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Animal Protocol |
Animal/Disease Models: Pregnant Wistar rats (12 weeks) [2]
Doses: 0.3 mg/kg, 1 mg/kg, 3 mg/kg Route of Administration: Oral Experimental Results: Dose-dependent inhibition of AUC glucose levels. |
References |
[1]. Y Sunaga, et al. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol. 2001 Nov 9;431(1):119-25.
[2]. Kiyoshi Ichikawa, et al. Effect of KAD-1229, a novel hypoglycaemic agent, on plasma glucose levels after meal load in type 2 diabetic rats. Clin Exp Pharmacol Physiol. May-Jun 2002;29(5-6):423-7. |
Molecular Formula |
C38H52CAN2O8
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Molecular Weight |
704.9061
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CAS # |
207844-01-7
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Related CAS # |
Mitiglinide calcium;145525-41-3;Mitiglinide;145375-43-5;Mitiglinide-d8 calcium hydrate
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SMILES |
[Ca+2].O=C(C([H])([H])[C@@]([H])(C(=O)[O-])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N1C([H])([H])[C@]2([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@]2([H])C1([H])[H].O=C(C([H])([H])[C@@]([H])(C(=O)[O-])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N1C([H])([H])[C@@]2([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@@]2([H])C1([H])[H].O([H])[H].O([H])[H]
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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 : ~25 mg/mL (~70.93 mM)
H2O : < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.09 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 (7.09 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4186 mL | 7.0931 mL | 14.1862 mL | |
5 mM | 0.2837 mL | 1.4186 mL | 2.8372 mL | |
10 mM | 0.1419 mL | 0.7093 mL | 1.4186 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.