| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. RT-PCR[2] Cell Line: | ||||||||||||
| In Vivo | Nateglinide (50mg/kg, orally in mice) stimulates human C-peptide secretion in the humanized mice and improved postprandial glucose concentrations[3]. Animal Model: | ||||||||||||
| Name | Nateglinide | ||||||||||||
| CAS | 105816-04-4 | ||||||||||||
| Formula | C19H27NO3 | ||||||||||||
| Molar Mass | 317.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Nateglinide
CAS: 105816-04-4 F: C19H27NO3 W: 317.42
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibi
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