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| Size | Price | Stock |
|---|---|---|
| 50mg | $55 | 3-6 Days |
| 100mg | $80 | 3-6 Days |
| 250mg | $120 | 3-6 Days |
| 500mg | $180 | 3-6 Days |
| 1g | $290 | 3-6 Days |
| 2g | $520 | 3-6 Days |
: Cat #: V2004 CAS #: 16208-51-8 Purity ≥ 98%
Description: Dimesna (also called BNP-7787) is an uroprotective agent used to decrease urotoxicity caused by anticancer drugs such cisplatin. It reacts with acrolein and other urotoxic metabolites of oxazaphosphorine class of antitumor drugs such as cyclophosphamide or ifosfamide to form stable, non-urotoxic compounds.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.
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| Molecular Weight (MW) | 326.34 |
|---|---|
| Molecular Formula | C4H8Na2O6S4 |
| CAS No. | 16208-51-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 65 mg/mL (199.2 mM) |
| Water: 65 mg/mL (199.2 mM) | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | Saline: 30 mg/mL |
| Synonyms | BNP-7787; BNP7787; BNP 7787; Tavocept |
| Protocol | In Vitro | In vitro activity: 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 | Tumors of urinary bladder induced by cyclophosphamide (CP) in rats can be significantly reduced by Dimesna administration in a dose-related manner. | |
| Animal model | CP treated Sprague-Dawley rats |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.0643 mL | 15.3214 mL | 30.6429 mL | 61.2858 mL |
| 5mM | 0.6129 mL | 3.0643 mL | 6.1286 mL | 12.2572 mL |
| 10mM | 0.3064 mL | 1.5321 mL | 3.0643 mL | 6.1286 mL |
| 20mM | 0.1532 mL | 0.7661 mL | 1.5321 mL | 3.0643 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.