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Other Sizes |
Purity: ≥98%
Mitiglinide (also known as KAD-1229; S21403) is a Potassiun Channel blocker that is used as a blood glucose-lowering drug, it stimulates insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells. Mitiglinide may be potential useful for the treatment of type 2 diabetes.
ln Vitro |
In COS-1 cells, mitigamininde reduces the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 of 100 nM), but even at high concentrations (more than 10 μM), it does not significantly inhibit the Kir6.2/SUR2A or Kir6.2/SUR2B channel currents[1].
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ln Vivo |
Up to five hours after a meal load, mitiglinide (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
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Molecular Weight |
315.41
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CAS # |
145375-43-5
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Related CAS # |
Mitiglinide calcium;145525-41-3;Mitiglinide calcium hydrate;207844-01-7;Mitiglinide-d8 calcium hydrate;(2R)-Mitiglinide-d5 calcium;Mitiglinide-d5 calcium
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SMILES |
O=C(O)[C@@H](CC1=CC=CC=C1)CC(N2C[C@]3([H])CCCC[C@]3([H])C2)=O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL | |
5 mM | 0.6341 mL | 3.1705 mL | 6.3410 mL | |
10 mM | 0.3170 mL | 1.5852 mL | 3.1705 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.