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KU14R Sale

(Synonyms: 2-(2-乙基-2,3-二氢-2-苯并呋喃基)-1H-咪唑,KU-14R;KU 14R) 目录号 : GC10626

KU14R 是一种新的 I(3)-R 拮抗剂,可选择性地阻断对咪唑啉的胰岛素分泌反应。

KU14R Chemical Structure

Cas No.:189224-48-4

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10mg
¥693.00
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50mg
¥3,087.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

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. 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.

Chemical Properties

Cas No. 189224-48-4 SDF
别名 2-(2-乙基-2,3-二氢-2-苯并呋喃基)-1H-咪唑,KU-14R;KU 14R
化学名 2-(2-ethyl-2,3-dihydrobenzofuran-2-yl)-1H-imidazole
Canonical SMILES CCC1(C2=NC=CN2)CC3=CC=CC=C3O1
分子式 C13H14N2O 分子量 214.26
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 4.6672 mL 23.3361 mL 46.6723 mL
5 mM 0.9334 mL 4.6672 mL 9.3345 mL
10 mM 0.4667 mL 2.3336 mL 4.6672 mL
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