Rotigaptide TFA(355151-12-1 free base) 是一种新型的 Cx43 特异性调节剂,是一种有效的 AAP。 Rotigaptide 可防止 Cx43 介导的间隙连接通讯的解偶联,并使急性代谢应激期间的细胞间通讯正常化。
产品描述
Rotigaptide TFA is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress.
体外活性
Rotigaptide TFA (100 nM; 24 hours) does not affect INS-1 cell apoptosis itself. Rotigaptide (100 nM; 24 hours) has a positive effect on the cycloheximide-mediated decrease in Cx43 protein levels in cultured neonatal ventricular myocytes. And it obviously decreases apoptosis in cytokine-exposed cells ~10% at IL-1b concentrations above 15 pg/ml in rat insulin-producing INS-1 cells [1][2].
体内活性
Rotigaptide TFA (intravenous administration; 300 mg/kg; single dose) treatment in mice and rats does not cause toxicity in either species. Rotigaptide (continuous intravenous infusion; 5-14 days) in rats (100 mg/kg) and dogs (10 mg/kg) is well tolerated and produces no compound-related effects or histological toxicological findings in escalating dose studies [3].
Cas No.
T16790L
分子式
C30H40F3N7O11
分子量
731.67
别名
Rotigaptide TFA
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years