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Dimesna

Catalog No.
A1652
Uroprotective agent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
100mg
$63.00
In stock
500mg
$171.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt326.34
Cas No.16208-51-8
FormulaC4H8Na2O6S4
Solubility≥16.35mg/mL in DMSO
Chemical Namedisodium;2-(2-sulfonatoethyldisulfanyl)ethanesulfonate
SDFDownload SDF
Canonical SMILESC(CS(=O)(=O)[O-])SSCCS(=O)(=O)[O-].[Na+].[Na+]
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description Dimesna is a kidney selective prodrug of Mesna with Km value of 636, 390 and 590 μM for OAT1, OAT3 and OAT4, resepectively.
Targets OAT1 OAT3 OAT4      
IC50 636 μM (Km) 390 μM (Km) 590 μM (Km)      

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