Gap 27是一种合成的 connexin43 模拟肽,是一种间隙连接抑制剂。它与通往第二跨膜连接蛋白区段的第二细胞外环的一部分具有保守的序列同源性。
产品描述
Gap 27 is a peptide(Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile) derived from connexin 43 that is a selective gap junction blocker.
体外活性
Gap 27 causes a remarked decrease in the number of both TRAP-positive mononuclear and multinucleated rat osteoclasts cultured on bovine bone slices. The activity of the remaining osteoclasts is found to be diminished by measuring the percentage of osteoclasts with actin rings of all TRAP-positive cells. In addition, the resorbed area in the treated cultures is greatly diminished[1]. Incubation of the carotid artery with the gap junction inhibitor Gap 27 (500 μM) essentially abolishes the hyperpolarization to acetylcholine but it is without effect on that to levcromakalim. Gap 27 inhibits acetylcholine-induced, endothelium-dependent hyperpolarizations in the guinea-pig-isolated internal carotid artery[2].
体内活性
Gap 27 (300 μM) inhibits relaxation by 40% in thoracic aorta and the superior mesenteric artery. Gap 27 also attenuates the endothelium-dependent component of the relaxation induced by ATP in thoracic aorta but did not modify force development in response to PhE[3].
Cas No.
198284-64-9
分子式
C60H101N15O17
分子量
1304.556
储存和溶解度
DMSO:Insoluble
H2O:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years