KU14R

Short Summary : I(3)-R antagonist

Category : Tyrosine Kinase|Insulin Receptor

Purity : 0.98

CAS Number : 189224-48-4

Formula : C13H14N2O

Molecular Weight : 214.26

SMILE : CCC1(C2=NC=CN2)CC3=CC=CC=C3O1

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : 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.

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