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In vitro: Polyoxyethylene stearate has been recommended as an additive to the radiolabelled 7H12 Middlebrook TB media and as such has been shown to enhance growth of mycobacteria in the radiometric BACTEC rapid culture system. Polyoxyethylene (50) stearate produces the greatest enhancement in growth and reduction in the time taken to detect growth for M. tuberculosis and polyoxyethylene (30) stearate and polyoxyethylene (JL) stearate for species of mycobacteria other than M. tuberculosis. Polyoxyethylene stearate inhibits P-gp mediated efflux in a concentration dependent manner mainly by modulating substrate-stimulated P-gp ATPase activity. Polyoxyethylene 40 stearate reduces vinblastine sulfate efllux. The cytotoxicity of vinblastine to K562/ADR cells is significantly enhanced when the cells are cotreated with 100 or 150 μg/mL polyoxyethylene 40 stearate. In vivo: Polyoxyethylene stearate is potentially useful as a pharmaceutical ingredient to improve the oral bioavailability of coadministered P-gp substrates and substrates for certain CYP isoforms. The average tumor volume and average tumor weight are significantly less in the polyoxyethylene 40 stearate + vinblastine group. The inhibition rate for tumor growth is increased from 0.06 (vinblastine group) to 0.84 (vinblastine+polyoxyethylene 40 stearate group).
| Cell Experiment | |
|---|---|
| Cell lines | Caco-2 cell line |
| Preparation method | Donor solutions of 200 ug/mL VBL with or without different concentrations of PS40 in TBS were added to the donor compartment. The nal concentrations of PS40 were 50, 100, and 150 ug/mL. The AP compartment and the BL compartment served as the donor compartments for absorptive (AP-BL) and ef ux (BL-AP) transport, respectively. |
| Concentrations | 50, 100, and 150 ug/mL. |
| Incubation time | 20, 40, 60, 90, 120, and 150 minutes |
| Animal Experiment | |
|---|---|
| Animal models | Female BALB/c-nu/nu mice |
| Formulation | 0.9% sodium chloride solution |
| Dosages | 150 ug/mL |
| Administration | i.v. |
| Molecular Weight | 725.0 |
| Formula | (C2H4O)10C18H36O2 |
| CAS Number | 9004-99-3 |
| Solubility (25°C) | 10mM in DMSO |
| 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.
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