Description: Kir6 (KATP) blocker; displays high affinity for SUR1/Kir6.2 channels
Alternative Names: A-4166, Senaglinide
Chemical Name:N-[[4-(1-Methylethyl)cyclohexyl]carbonyl]-D-phenylalanine
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Kir6 (KATP) blocker. Exhibits in vitro tissue selectivity for pancreatic β-cell-type Kir6 channels over cardiovascular Kir6 channels; displays high affinity for SUR1/Kir6.2 channels. Hypoglycemic agent; stimulates insulin secretion from pancreatic β-cells by increasing cytosolic Ca2+ concentration. Also agonist at the orphan receptor MRGPRX4.
Compound Libraries
Nateglinide is also offered as part of the
Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
31.74
100
Preparing Stock Solutions
The following data is based on the product molecular weight 317.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
3.15 mL
15.75 mL
31.5 mL
5 mM
0.63 mL
3.15 mL
6.3 mL
10 mM
0.32 mL
1.58 mL
3.15 mL
50 mM
0.06 mL
0.32 mL
0.63 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Shinkaiet al (1989) N-(cyclohexylcarbonyl)-D-phenylalanines and related compounds. A new class of hypoglycemic agents. J.Med.Chem. 32 1436 PMID: 2738878
Fujitaniet al (1997) The ability of a new hypoglycemic agent, A-4166, compared to sulphonylureas, to increase cytosolic Ca2+ in pancreatic beta-cells under metabolic inhibition. Br.J.Pharmacol. 120 1191 PMID: 9105692
Huet al (1999) Tissue selectivity of antidiabetic agent nateglinide: study on cardiovascular and β-cell KATP channels. J.Pharmacol.Exp.Ther. 291 1372 PMID: 10565863
Chachinet al (2003) Nateglinide, a D-phenylalanine derivative lacking either a sulfonylurea or benzamido moiety, specifically inhibits pancreatic β-cell-type KATP channels. J.Pharmacol.Exp.Ther. 304 1025 PMID: 12604678
Kroezeet al (2015) PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nat.Struct.Mol.Biol. 22 362 PMID: 25895059