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- Dimesna 16208-51-8

- Dimesna 16208-51-8
Dimesna 16208-51-8
产品描述 描述 Dimesna is an uroprotective agent used to decrease urotoxicity.
纯度 98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 地美si钠;BNP-7787外观 白色粉末可溶性/溶解性 DMSO :60 mg/mL (183.9 mM)
Water :60 mg/mL (183.9 mM)生物活性 In vitro(体外研究) Dimesna modulates paclitaxel-induced hyperpolymerization of MTP in a dose-dependent manner, and mesna, an in vivo metabolite of Dimesna, protects against time-dependent cisplatin-induced inactivation of MTP. Dimesna -mediated prevention or mitigation of cisplatin-induced nephrotoxicity may involve aminopeptidase N (APN) inhibition by certain Dimesna -derived esna-disulfide heteroconjugates and appears correlated to the presence of a glycinate moiety and/or an anionic group. Two general mechanisms for Dimesna -mediated nephroprotection of cisplatin-induced nephrotoxicity involving the gamma-glutamyl transpeptidase (GGT), APN and cysteine-conjugated-β-lyase (CCBL) nephrotoxigenic pathway are proposed which acting in a concerted and/or synergistic manner, and thereby prevent or mitigate cisplatin-induced renal toxicity. Mesna and its dimer, Dimesna, are coadministered for mitigation of ifosfamide- and cisplatin-induced toxicities, respectively. Dimesna is selectively reduced to mesna in the kidney, producing its protective effects. In vitro screens of uptake and efflux transporters reveal renal organic anion transporters OAT1, OAT3, and OAT4 are responsible for kidney-specific uptake of Dimesna. Uptake of Dimesna by OAT1, OAT3, and OAT4 is determined to be saturable with KM of 636 μM, 390 μM and 590 μM, respectively.In vivo(体内研究) Tumors of urinary bladder induced by cyclophosphamide (CP) in rats can be significantly reduced by Dimesna administration in a dose-related manner.参考文献 参考文献 1. Parker AR, et al. Mol, Cancer Ther, 2010, 9(9), 2558-2567.
2. Hausheer FH, et al. Cancer Chemother Pharmacol, 2010, 65(5), 941-951.
研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryDimesna 16208-51-8温馨提示:本产品仅作科研实验使用,不支持临床等研究
