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.
For the detailed information of KU14R, the solubility of KU14R in water, the solubility of KU14R in DMSO, the solubility of KU14R in PBS buffer, the animal experiment (test) of KU14R, the cell expriment (test) of KU14R, the in vivo, in vitro and clinical trial test of KU14R, the EC50, IC50,and Affinity of KU14R, Please contact DC Chemicals. |