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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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Nateglinide 化学構造

Cas No.: 105816-04-4

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10mM (in 1mL DMSO)
$32.00
在庫あり
10mg
$45.00
在庫あり
25mg
$77.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of Nateglinide

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.

Chemical Properties of Nateglinide

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Nateglinide

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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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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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Average Rating: 5 ★★★★★ (Based on Reviews and 35 reference(s) in Google Scholar.)

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