Reversan is a selective inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp). Reversan increases the sensitivity of MRP1-overexpressing tumor cells (MCF7/VP) to doxorubicin, vincristine and etoposide by 3.8-, 14.6- and 11.6-fold respectively. Reversan increases the efficacy of vincristine and etoposide in murine models of neuroblastoma in vivo.
| Molecular Weight | 441.52 |
| Formula | C26H27N5O2 |
| CAS Number | 313397-13-6 |
| Solubility (25°C) | DMSO 11 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related P-glycoprotein Products |
|---|
| Reversin 121
Reversin 121 is a P-glycoprotein inhibitor. |
| Reversin 205
Reversin 205 ([Boc-Glu(Obzl)]2-Lys-Ome) is a P-glycoprotein (ABCB1) inhibitor. |
| P-gb-IN-1
P-gb-IN-1 inhibitor. |
| P-gp inhibitor 13
P-gp inhibitor 13 is a P-gp inhibitor. |
| ABCB1-IN-1
ABCB1-IN-1 is a potent ABCB1 inhibitor. |
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