Nateglinide - CAS 105816-04-4
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Not Intended for Therapeutic Use. For research use only.
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Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the β cells.
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1.Effects of nateglinide and rosiglitazone on pancreatic alpha- and beta-cells, GLP-1 secretion and inflammatory markers in patients with type 2 diabetes: randomized crossover clinical study.
Tostes GC1, Cunha MR1, Fukui RT1, Correia MR1, Rocha DM1, Dos Santos RF1, da Silva ME1. Diabetol Metab Syndr. 2016 Jan 4;8:1. doi: 10.1186/s13098-015-0120-6. eCollection 2016.
BACKGROUND: To compare the effects of nateglinide and rosiglitazone on inflammatory markers, GLP-1 levels and metabolic profile in patients with type 2 diabetes (DM2).
2.Comparison of sitagliptin with nateglinide on postprandial glucose and related hormones in drug-naïve Japanese patients with type 2 diabetes mellitus: A pilot study.
Tanimoto M1, Kanazawa A2, Hirose T1, Yoshihara T1, Kobayashi-Kimura S1, Nakanishi R1, Tosaka Y1, Sasaki-Omote R1, Kudo-Fujimaki K1, Komiya K1, Ikeda F1, Someya Y1, Mita T1, Fujitani Y1, Watada H3. J Diabetes Investig. 2015 Sep;6(5):560-6. doi: 10.1111/jdi.12338. Epub 2015 Mar 15.
AIMS/INTRODUCTION: Dipeptidyl peptidase-4 inhibitors and glinides are effective in reducing postprandial hyperglycemia. However, little information is available on the comparative effects of the two drugs on the levels of postprandial glucose. The aim of the present study was to compare the effects of sitagliptin and nateglinide on meal tolerance tests in drug-naïve patients with type 2 diabetes mellitus.
3.Preparation of polyclonal antibodies for nateglinide (NTG) and development of a sensitive chemiluminescent immunoassay to detect NTG in tablets and serum.
Zheng L1, Wang J1, Zhang J2, Song Z1, Dong Y1, Wang Y1, Tong Z2, Deng C3, Yin Y1, Meng M4, Xi R1. Talanta. 2016 Jan 1;146:483-9. doi: 10.1016/j.talanta.2015.09.008. Epub 2015 Sep 9.
In this study, we prepared polyclonal antibodies against anti-diabetic drug nateglinide (NTG), and established a sensitive chemiluminescent immunoassay (CLIA) to detect NTG in tablets and serum. Two kinds of immunogens were synthesized using ethylcarbodiimide (EDC)/hydroxysuccinimide (NHS) and carbonyldiimidazole (CDI)/4-dimethylaminopyridine (DMAP) as coupling reagents respectively. When activated by EDC/NHS, more molecules of NTG coupled with carrier protein in immunogens. A horseradish peroxidase (HRP)-luminol-H2O2 system with p-iodophenol enhancement was applied in the CLIA analysis. The antibodies in EDC/NHS group showed higher titer, sensitivity and wider detection linear range than those in CDI/DMAP group, and were chosen for next studies. The developed CLIA assay exhibited good selectivity towards NTG among structually similar analogs. The method could detect as low as 0.35 ng mL(-1) NTG in buffer, 2.1 ng mL(-1) NTG in serum and 0.
4.Development and in vitro/in vivo evaluation of controlled release provesicles of a nateglinide-maltodextrin complex.
Sahoo RK1, Biswas N1, Guha A1, Sahoo N1, Kuotsu K1. Acta Pharm Sin B. 2014 Oct;4(5):408-16. doi: 10.1016/j.apsb.2014.08.001. Epub 2014 Sep 4.
The aim of this study was to characterize the provesicle formulation of nateglinide (NTG) to facilitate the development of a novel controlled release system of NTG with improved efficacy and oral bioavailability compared to the currently marketed NTG formulation (Glinate™ 60). NTG provesicles were prepared by a slurry method using the non-ionic surfactant, Span 60 (SP), and cholesterol (CH) as vesicle forming agents and maltodextrin as a coated carrier. Multilamellar niosomes with narrow size distribution were shown to be successfully prepared by means of dynamic laser scattering (DLS) and field emission scanning electron microscopy (FESEM). The absence of drug-excipient interactions was confirmed by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. In vitro release of NTG in different dissolution media was improved compared to pure drug. A goat intestinal permeation study revealed that the provesicular formulation (F4) with an SP:CH ratio of 5:5 gave higher cumulative amount of drug permeated at 48 h compared to Glinate™ 60 and control.
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CAS 105816-04-4 Nateglinide

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