BMS-806 (BMS 378806) is a small molecules gp120/CD4 inhibitor with an IC50 of median 5 nM. BMS-806 (BMS 378806) was proved to be specific for HIV-1, with no activity against HIV-2 or simian immunodeficiency virus. BMS-806 (BMS 378806) is active against HIV-1 isolates irrespective of chemokine receptor preference (23, 24). BMS-806 (BMS 378806) binds gp120, and changes in particular gp120 amino acid residues can alter the sensitivity of the virus to BMS-806 (BMS 378806). BMS-806 (BMS 378806) potently inhibited HIV-1 infection regardless of the particular chemokine receptor used.
| Cell Experiment | |
|---|---|
| Cell lines | MT-2 cells |
| Preparation method | To determine cytotoxicity, MT-2 cells are incubated in the presence of serially diluted BMS-806 for 6 days and cell viability is quantitated using an XTT [2,3-bis(2-methoxy-4-nitro-5-sulfophenyl-2H-tetrazolium-5-carboxanilide] assay to calculate the 50% cytotoxic concentrations (CC50s). |
| Concentrations | 0-3 mM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | Rat, dog and monkey |
| Formulation | BMS-806 is dissolved in poly (ethylene glycol) 400/ethanol (90:10 v/v). |
| Dosages | 5 mg/kg, 3.4 mg/kg and 3.4 mg/kg. |
| Administration | BMS-806 is intravenously administered. |
| Molecular Weight | 406.43 |
| Formula | C22H22N4O4 |
| CAS Number | 357263-13-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 80 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.
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