Kuwanon H 是分离自桑白皮的黄酮类化合物,具有拮抗非肽类蛙皮素受体的活性。Kuwanon H 特异性抑制细胞内胃泌激素释放肽 CRP 与GRP-preferring 受体的结合,Ki为 290 nM。
产品描述
Kuwanon H is a specific antagonist for the gastrin-releasing peptide (GRP) -preferring receptor with Ki values of 290 nM and can be useful for studying the physiological and pathological role of GRP. Kuwanon H is a potent non-peptide bombesin receptor antagonist.
体外活性
Kuwanon G and H, isolated from the methanol extract of Morus bombycis, inhibited specific binding of [125I]gastrin-releasing peptide (GRP) to GRP-preferring receptors in murine Swiss 3T3 fibroblasts with Ki values of 470 and 290 nM, respectively. Kuwanon H was one order of magnitude less potent for inhibiting [125I]bombesin binding to neuromedin B (NMB)-preferring receptors in rat esophagus membranes. This compound antagonized bombesin-induced increases in the cytosolic free calcium concentration and GRP-induced DNA synthesis in Swiss 3T3 cells.
Cas No.
76472-87-2
分子式
C45H44O11
分子量
760.82
储存和溶解度
DMSO:50 mg/mL (65.72 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years