Nateglinide (Synonyms: A-4166, SDZ-DJN 608) |
カタログ番号GC10091 |
D-フェニルアラニン誘導体であるナテグリニドは、経口活性で短時間作用型のインスリン分泌促進剤であり、DPP IV 阻害剤です。
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Cas No.: 105816-04-4
Sample solution is provided at 25 µL, 10mM.
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
Nateglinide inhibits typical recordings of dinitrophenol-induced KATP currents in a concentration-dependent manner. Nateglinide exhibits IC50 values of 7.4 μM and 2.4 μM for 5 mM glucose (G5) and 16 mM (G16) glucose, respectively[2].
Nateglinide (50mg/kg, orally in mice) stimulates human C-peptide secretion in the humanized mice and improved postprandial glucose concentrations[3].
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.
Cas No. | 105816-04-4 | SDF | |
同義語 | A-4166, SDZ-DJN 608 | ||
Chemical Name | (2R)-3-phenyl-2-[(4-propan-2-ylcyclohexanecarbonyl)amino]propanoic acid | ||
Canonical SMILES | CC(C)C1CCC(CC1)C(=O)NC(CC2=CC=CC=C2)C(=O)O | ||
Formula | C19H27NO3 | M.Wt | 317.42 |
溶解度 | ≥ 16.4mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.1504 mL | 15.752 mL | 31.504 mL |
5 mM | 0.6301 mL | 3.1504 mL | 6.3008 mL |
10 mM | 0.315 mL | 1.5752 mL | 3.1504 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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