Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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5g |
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Other Sizes |
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Purity: ≥98%
Mitiglinide Calcium (formerly KAD-1229; S-21403; KAD1229; S21403; Glufast), the calcium salt of Mitiglinide, is a potassiun channel blocker that has been approved as a blood glucose-lowering drug for the treatment of type 2 diabetes. It acts by stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
ln Vitro |
Mitiglinide Calcium reduces the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 μM) in COS-1 cells[1].
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ln Vivo |
Up to five hours after a meal load, mitiglinide calcium (1-3 mg/kg; po) inhibits both the rise in plasma glucose levels observed following the meal load and the area under the curve for plasma glucose levels (AUCglucose).
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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 administration Experimental Results: Dose-dependently suppressed AUCglucose 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 |
(C19H24NO3)2.CA
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Molecular Weight |
668.88
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CAS # |
145525-41-3
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Related CAS # |
Mitiglinide calcium hydrate;207844-01-7;Mitiglinide;145375-43-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C([O-])C(CC1=CC=CC=C1)CC(N2C[C@]3([H])CCCC[C@]3([H])C2)=O.O=C([O-])C(CC4=CC=CC=C4)
CC(N5C[C@]6([H])CCCC[C@]6([H])C5)=O.[Ca+2] |
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Synonyms |
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.50 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 5.0 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: ≥ 0.5 mg/mL (1.50 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 5.0 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: ≥ 0.5 mg/mL (1.50 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 | 1.4950 mL | 7.4752 mL | 14.9504 mL | |
5 mM | 0.2990 mL | 1.4950 mL | 2.9901 mL | |
10 mM | 0.1495 mL | 0.7475 mL | 1.4950 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.