KU14R

Modify Date: 2024-01-08 17:53:59

KU14R Structure
KU14R structure
Common Name KU14R
CAS Number 189224-48-4 Molecular Weight 214.263
Density 1.2±0.1 g/cm3 Boiling Point 428.1±34.0 °C at 760 mmHg
Molecular Formula C13H14N2O Melting Point 137-139ºC
MSDS N/A Flash Point 154.4±15.9 °C

 Use of KU14R


KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.IC50 Value:Target: Insulin ReceptorA 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.

 Names

Name 2-(2-ethyl-3H-1-benzofuran-2-yl)-1H-imidazole
Synonym More Synonyms

 KU14R Biological Activity

Description KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.IC50 Value:Target: Insulin ReceptorA 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.
Related Catalog
References

[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. 2

[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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 428.1±34.0 °C at 760 mmHg
Melting Point 137-139ºC
Molecular Formula C13H14N2O
Molecular Weight 214.263
Flash Point 154.4±15.9 °C
Exact Mass 214.110611
PSA 37.91000
LogP 2.10
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.595
Storage condition Store at RT

 Synonyms

cs-1007
1H-Imidazole, 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-
hms3267m22
ku14r
2-(2-Ethyl-2,3-dihydro-1-benzofuran-2-yl)-1H-imidazole
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