Catalog Number: 4231
Alternate Names: A-4166, Senaglinide
Chemical Name: N-[[4-(1-Methylethyl)cyclohexyl]carbonyl]-D-phenylalanine
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.
Technical Data
  • M.Wt:
    317.42
  • Formula:
    C19H27NO3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Storage:
    Store at RT
  • CAS No:
    105816-04-4
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.
Background References
  1. The ability of a new hypoglycemic agent, A-4166, compared to sulphonylureas, to increase cytosolic Ca2+ in pancreatic beta-cells under metabolic inhibition.
    Fujitani et al.
    Br.J.Pharmacol., 1997;120:1191
  2. Tissue selectivity of antidiabetic agent nateglinide: study on cardiovascular and β-cell KATP channels.
    Hu et al.
    J.Pharmacol.Exp.Ther., 1999;291:1372
  3. Nateglinide, a D-phenylalanine derivative lacking either a sulfonylurea or benzamido moiety, specifically inhibits pancreatic β-cell-type KATP channels.
    Chachin et al.
    J.Pharmacol.Exp.Ther., 2003;304:1025
  4. N-(cyclohexylcarbonyl)-D-phenylalanines and related compounds. A new class of hypoglycemic agents.
    Shinkai et al.
    J.Med.Chem., 1989;32:1436
  5. PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome.
    Kroeze et al.
    Nat.Struct.Mol.Biol., 2015;22:362

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