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CAS No. : 189224-48-4
Biological Activity：KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.
Target: 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. 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.
Research Area：Metabolic Disease|Endocrinology
Related Small Molecules:AGL-2263;SU4984;HNMPA-(AM)3;S961 TFA;OI338;Gastric Inhibitory Peptide, porcine;MSDC 0160;[Tyr0] Gastric Inhibitory Peptide (23-42), human;AVJ16;GIP, human;GSK1838705A;DA-JC4;MSDC-0602K;AG1024;MID-1;(Pro3) GIP, human;HNMPA;BMS-754807;GSK1904529A;NVP-ADW742;Linsitinib-d3;GIP (1-30) amide,human acetate
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