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KU14R

Catalog No. T15672 CAS 189224-48-4

KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.

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KU14R, CAS 189224-48-4

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 970.00 $ 776.00
50 mg	6-8 weeks	$ 1,980.00 $ 1,584.00
100 mg	6-8 weeks	$ 2,500.00 $ 2,000.00

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Purity: 98%

Biological Description

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Description

KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.

In vitro

KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP). 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. By measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c), and dynamic insulin secretion to compare the effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells. KU14R (30, 100 or 300 micromol/l) was ineffective, in the presence of 10 mmol/l but not of 5 mmol/l glucose. 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.

Molecular Weight	214.26
Formula	C13H14N2O
CAS No.	189224-48-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Keywords

KU14R 189224-48-4 Others KU-14R inhibitor inhibit

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