| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
The primary targets of Reversan are the ATP-binding cassette (ABC) transporters MRP1 (ABCC1) and P-glycoprotein (P-gp/ABCB1). These transporters are responsible for the efflux of a wide range of chemotherapeutic drugs from cancer cells, leading to multidrug resistance. By inhibiting these transporters, Reversan prevents the efflux of drugs, thereby increasing their intracellular concentration and restoring their efficacy. It is also an inhibitor of MRP5.
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| ln Vitro |
In vitro, Reversan is a potent and nontoxic inhibitor of MRP1 and P-gp function. It is six to eight times more potent than other known drug transporter inhibitors. It increases the sensitivity of multidrug-resistant cancer cells to chemotherapeutic agents by inhibiting drug efflux. It is used in cell-based assays to demonstrate the reversal of multidrug resistance, showing that it can restore the cytotoxic effects of drugs like vincristine and etoposide in resistant cell lines.
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| ln Vivo |
In vivo, Reversan has been shown to increase the efficacy of chemotherapeutic agents. It increases the efficacy of etoposide in murine models of neuroblastoma. By inhibiting drug efflux transporters, it enhances the accumulation of chemotherapeutic drugs in tumor tissues, leading to improved anti-tumor activity. Its non-toxic profile makes it a promising candidate for combination therapy to overcome multidrug resistance in cancer.
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| Enzyme Assay |
Cell-free assays for Reversan typically assess its inhibition of transporter function. A common protocol involves using inside-out membrane vesicles prepared from cells overexpressing MRP1 or P-gp. The vesicles are incubated with a fluorescent or radiolabeled substrate (e.g., [3H]-vinblastine or [3H]-methotrexate) and varying concentrations of Reversan. The accumulation of the substrate inside the vesicles is measured. The IC50 is determined from the dose-response curve. This assay directly measures the compound's ability to inhibit the transporter's efflux activity.
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| Cell Assay |
For in vitro cellular experiments, multidrug-resistant cancer cell lines (e.g., MCF7/VP, which overexpresses MRP1) are cultured in appropriate media. Cells are treated with a chemotherapeutic agent (e.g., doxorubicin, vincristine) in the presence or absence of Reversan at various concentrations (typically 0.1-10 uM). Cell viability is assessed using MTT or resazurin assays. The reversal of resistance is demonstrated by a significant decrease in the IC50 of the chemotherapeutic agent when combined with Reversan.
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| Animal Protocol |
In vivo animal experiments with Reversan are conducted in murine models of cancer, such as neuroblastoma xenografts. A common protocol involves implanting multidrug-resistant tumor cells into mice. Once tumors are established, the animals are treated with a chemotherapeutic agent (e.g., etoposide) alone or in combination with Reversan (e.g., 10-50 mg/kg, IP). Tumor growth is monitored by caliper measurements. The combination therapy is expected to show significantly greater tumor growth inhibition than the chemotherapeutic agent alone.
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| ADME/Pharmacokinetics |
Reversan has a molecular weight of 379.43 g/mol and a molecular formula of C22H21N5O. It is a small molecule that is likely to have good oral bioavailability. It is soluble in DMSO. For in vivo studies, it can be formulated in a vehicle such as DMSO, PEG300, or saline. It should be stored as a powder at -20degC, protected from light and moisture. Its pharmacokinetic properties, including half-life and tissue distribution, would need to be characterized for therapeutic development.
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| Toxicity/Toxicokinetics |
Reversan is a nontoxic inhibitor of MRP1 and P-gp function. Its non-toxic profile is a key feature that distinguishes it from other transporter inhibitors. It is six to eight times more potent than verapamil and other inhibitors. It is well-tolerated in animal models at doses that effectively reverse drug resistance. It is for research use only and not for human therapeutic use. It should be handled with standard laboratory precautions.
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| References |
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| Additional Infomation |
Reversan is a potent, nontoxic inhibitor of the multidrug resistance transporters MRP1 and P-gp. It is used to overcome transporter-mediated chemoresistance in cancer research. It is six to eight times more potent than verapamil and increases the efficacy of chemotherapeutic agents like vincristine and etoposide. It has shown efficacy in murine models of neuroblastoma. It is a valuable research tool for studying multidrug resistance.
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| Molecular Formula |
C26H27N5O2
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|---|---|
| Molecular Weight |
441.524885416031
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| Exact Mass |
441.216
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| CAS # |
313397-13-6
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| PubChem CID |
2298706
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.028
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
616
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JTRXWCLQFAZHGP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H27N5O2/c32-26(27-12-7-13-30-14-16-33-17-15-30)22-19-28-31-24(21-10-5-2-6-11-21)18-23(29-25(22)31)20-8-3-1-4-9-20/h1-6,8-11,18-19H,7,12-17H2,(H,27,32)
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| Chemical Name |
N-(3-morpholin-4-ylpropyl)-5,7-diphenylpyrazolo[1,5-a]pyrimidine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~13 mg/mL (~29.44 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.56 mg/mL (3.53 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 15.6 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2649 mL | 11.3245 mL | 22.6490 mL | |
| 5 mM | 0.4530 mL | 2.2649 mL | 4.5298 mL | |
| 10 mM | 0.2265 mL | 1.1325 mL | 2.2649 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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