Dimesna
(Synonyms: 地美司钠; BNP-7787) 目录号 : GC16262Dimesna 是一种用于降低尿毒症的保护剂。
Cas No.:16208-51-8
Sample solution is provided at 25 µL, 10mM.
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Dimesna is an inhibitor of OAT family with IC50 value of 636 μM, 390 μM, and 590 μM for OAT1, OAT3, and OAT4, respectively [1].
OATs (organic anion transporters) involve in many life processes, like elimination of a variety of endogenous substances, xenobiotics and their metabolites from the body. It has been shown that OATs play an important role in mediating the renal and hepatic elimination of organic anions using molecular cloning method [2].
Dimesna is an OAT inhibitor and often used as an uroprotective drug. When tested with renal tubular cell line LLC-PK1, in combination with IF metabolites, dimesna treatment exerted uroprotective action [3]. When tested with human renal proximal tubule HK-2 cells, dimesna was detected to accumulate in cells and played an important role in reducing chemotherapy-induced toxicities [4].
References:
[1].Cutler, M.J., et al., In vitro and in vivo assessment of renal drug transporters in the disposition of mesna and dimesna. J Clin Pharmacol, 2012. 52(4): p. 530-42.
[2].Roth, M., A. Obaidat, and B. Hagenbuch, OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies. Br J Pharmacol, 2012. 165(5): p. 1260-87.
[3].Mohrmann, M., et al., Dithio-bis-mercaptoethanesulphonate (DIMESNA) does not prevent cellular damage by metabolites of ifosfamide and cyclophosphamide in LLC-PK1 cells. Pediatr Nephrol, 1994. 8(4): p. 458-65.
[4].Hausheer, F.H., et al., Accumulation of BNP7787 in human renal proximal tubule cells. J Pharm Sci, 2011. 100(9): p. 3977-84.
Cas No. | 16208-51-8 | SDF | |
别名 | 地美司钠; BNP-7787 | ||
化学名 | disodium;2-(2-sulfonatoethyldisulfanyl)ethanesulfonate | ||
Canonical SMILES | C(CS(=O)(=O)[O-])SSCCS(=O)(=O)[O-].[Na+].[Na+] | ||
分子式 | C4H8Na2O6S4 | 分子量 | 326.34 |
溶解度 | ≥ 16.35mg/mL in DMSO | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.0643 mL | 15.3214 mL | 30.6429 mL |
5 mM | 0.6129 mL | 3.0643 mL | 6.1286 mL |
10 mM | 0.3064 mL | 1.5321 mL | 3.0643 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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