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10mg |
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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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Purity: ≥98%
Nateglinide (formerly A-4166; trade names: Fastic, Starlix), a meglitinide analog, is a potent and orally bioavailable antihyperglycemic medication used for treating type 2 diabetes [non-insulin-dependent diabetes mellitus (NIDDM)]. It lowers blood glucose levels by acting as an insulin secretagog agent which stimulates insulin secretion from the pancreas. It is a short-acting insulin secretagogue that inhibits ATP-sensitive K+ channels in pancreatic β-cells, which depolarizes the β cells and opens voltage-gated calcium channels, leading to calcium influx and fusion of insulin-containing vesicles with the cell membrane, and insulin secretion occurs.
ln Vitro |
In a concentration-dependent manner, nateglinide blocks typical recordings of dinitrophenol-induced KATP currents. For 5 mM (G5) and 16 mM (G16) glucose, nateglinide has IC50 values of 7.4 μM and 2.4 μM, respectively[2].
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ln Vivo |
Oral administration of nateglinide (50 mg/kg) to mice results in increased postprandial glucose concentrations and stimulation of human C-peptide production in the humanized mice[3].
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Cell Assay |
Cell Types: Rat pancreatic β-cells.
Tested Concentrations: 0-100 μM. Incubation Duration: ~20 min. Experimental Results: Produced a complete inhibition of KATP current at concentration of 3 μM. |
Animal Protocol |
Animal/Disease Models: Mice[3].
Doses: 50mg/kg. Route of Administration: Orally at 60min before oral administration of 4 g/kg glucose. Experimental Results: Stimulates human C-peptide secretion. |
References |
[1]. Christopher J. Dunn, et al. Nateglinide. OFILE Drugs 2000 Sep: 60 (3): 6.
[2]. Shiling Hu, et al. Interaction of nateglinide with KATP channel in h-cells underlies its unique insulinotropic action. European Journal of Pharmacology. 442 (2002) 163-171. [3]. Jian Luo, et al. Evaluating insulin secretagogues in a humanized mouse model with functional human islets. Metabolism. 2013 Jan;62(1):90-9. [4]. Duffy NA, et al. Effects of antidiabetic drugs on dipeptidyl peptidase IV activity: nateglinide is an inhibitor of DPP IV and augments the antidiabetic activity of glucagon-like peptide-1. Eur J Pharmacol. 2007 Jul 30;568(1-3):278-86. |
Molecular Formula |
C19H27NO3
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Molecular Weight |
317.42
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CAS # |
105816-04-4
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Related CAS # |
Nateglinide-d5;1227666-13-8
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SMILES |
O=C(C1([H])C([H])([H])C([H])([H])C([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])C1([H])[H])N([H])[C@@]([H])(C(=O)O[H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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InChi Key |
OELFLUMRDSZNSF-BRWVUGGUSA-N
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InChi Code |
InChI=1S/C19H27NO3/c1-13(2)15-8-10-16(11-9-15)18(21)20-17(19(22)23)12-14-6-4-3-5-7-14/h3-7,13,15-17H,8-12H2,1-2H3,(H,20,21)(H,22,23)/t15-,16-,17-/m1/s1
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Chemical Name |
(R)-2-((1r,4R)-4-isopropylcyclohexanecarboxamido)-3-phenylpropanoic acid
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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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1504 mL | 15.7520 mL | 31.5040 mL | |
5 mM | 0.6301 mL | 3.1504 mL | 6.3008 mL | |
10 mM | 0.3150 mL | 1.5752 mL | 3.1504 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00858013 | Completed Has Results | Drug: Nateglinide Drug: Glimepiride |
Type 2 Diabetes Mellitus | Ajou University School of Medicine | April 24, 2009 | Phase 4 |
NCT01160029 | Completed | Drug: Nateglinide | Healthy | Dr. Reddy's Laboratories Limited | October 2004 | Phase 1 |
NCT01159158 | Recruiting | Drug: Larotrectinib Sulfate Procedure: Bone Scan |
Recurrent Glioma Refractory Glioma |
Dr. Reddy's Laboratories Limited | February 2007 | Phase 1 |
NCT00928889 | Completed Has Results | Drug: Nateglinide 120 mg Drug: Acarbose 50 mg |
Diabetes Mellitus, Type 2 | Novartis Pharmaceuticals | July 2009 | Phase 4 |