KU14R

KU14R is a new I (3) -R antagonist, which selectively blocks the insulin secretory response to imidazolines. IC50 Value: Target: Insulin Receptor A new I (3) -R antagonist, KU14R (2 (2-ethyl 2,3-dihydro-2-benzofuranyl) -2-imidazole), which selectively blocks the insulin secretory response to imidazolines. KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP) . The effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells was compared by measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c) and dynamic insulin secretion. In the presence of 10 mmol/l but not of 5 mmol/l glucose, KU14R (30, 100 or 300 micromol/l) was ineffective. KATP channel was blocked by KU14R (IC50 31.9 micromol/l, Hill slope -1.5) . KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.

Product Specifications

CAS Number

[189224-48-4]

UNSPSC

12352005

Target

Insulin Receptor

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/ku14r.html

Purity

98.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CCC1(C2=NC=CN2)OC3=CC=CC=C3C1

Molecular Formula

C13H14N2O

Molecular Weight

214.26

References & Citations

[1]Bozdagi O, Wang XB, Martinelli GP, et al. Imidazoleacetic acid-ribotide induces depression of synaptic responses in hippocampus through activation of imidazoline receptors. J Neurophysiol. 2011,105 (3) :1266-75.|[2]Bleck C, Wienbergen A, Rustenbeck I. Essential role of the imidazoline moiety in the insulinotropic effect but not the KATP channel-blocking effect of imidazolines; a comparison of the effects of efaroxan and its imidazole analogue, KU14R. Diabetologia. 2005 Dec;48 (12) :2567-75.|[3]Cooper EJ, Hudson AL, Parker CA, et al. Effects of the beta-carbolines, harmane and pinoline, on insulin secretion from isolated human islets of Langerhans. Eur J Pharmacol. 2003;482 (1-3) :189-96.|[4]Mayer G, Taberner PV. Effects of the imidazoline ligands efaroxan and KU14R on blood glucose homeostasis in the mouse. Eur J Pharmacol. 2002;454 (1) :95-102.|[5]Susan L.F Chana, Anna L Palletta, John Clewsb. Evidence that the ability of imidazoline compounds to stimulate insulin secretion is not due to interaction with σ receptors. European Journal of Pharmacology. 1997,323 (2-3) : 241-244.