CAS 189224-48-4|KU14R

Introduction：Basic information about CAS 189224-48-4|KU14R, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. KU14R BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

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	/	Flash Point	154.4±15.9 °C

Names

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

KU14R BiologicalActivity

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	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>Insulin ReceptorResearch Areas >>Metabolic Disease
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.

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

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>Insulin ReceptorResearch Areas >>Metabolic Disease

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
InChIKey	JCWVNNMJXQJVNC-UHFFFAOYSA-N
SMILES	CCC1(c2ncc[nH]2)Cc2ccccc2O1
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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