Dimesna - 10mM in DMSO , CAS No.16208-51-8

CAS: 16208-51-8 Cat. No.: D408615 Molecular Weight: 326.34 EC Number: 240-337-2

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Dimesna (BNP-7787) is anuroprotective agentused to decrease urotoxicity.
In vitro

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. ^[1] 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. ^[2] 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 K_M of 636 μM, 390 μM and 590 μM, respectively. ^[3]

In vivo

Tumors of urinary bladder induced by cyclophosphamide (CP) in rats can be significantly reduced by Dimesna administration in a dose-related manner. ^[4]
Cell Data

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Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Kidney selective (K M values are 636, 390 and 590 μM for OAT1, OAT3, and OAT4 resepectively) prodrug to Mesna. Shows uroprotective effects against nephrotoxic agents in vivo . Orally active.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: C(CS(=O)(=O)[O-])SSCCS(=O)(=O)[O-].[Na+].[Na+]
• Molecular Weight: 326.34
• Reaxy-Rn: 6494921
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6494921&ln=