MDL-860 is a 5-nitro-2-phenoxybenzonitrile that exerts broad-spectrum antipicornaviral activity (MIC50 from 0.1-1.5 μg/mL in HeLa cultures) by acting as an irreversible inhibitor against host phosphatidylinositol-4 kinase beta (PI4KB; PtdIns 4-kinase beta; PI4Kbeta; NPIK; PI4K92) via covalent modification of Cys646 located at the bottom of a surface pocket apart from the PI4KB active site. MCL-860 (MIC50 from 0.1-1.5 μg/mL in HeLa cultures). A pleconaril/MDL-860/oxoglaucine consecutive alternating administration (CAA), but not simultaneous daily treatment, is reported to be effective against coxsackievirus B1 infection without the development of drug resistance in newborn mice (75 mg/kg MDL-860 via s.c. every third day on the day following pleconaril and prior to oxoglaucine).
| Molecular Weight | 309.1 |
| Formula | C13H6Cl2N2O3 |
| CAS Number | 78940-62-2 |
| Solubility (25°C) | DMSO: 2 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.
[2] Georgi M Dobrikov, et al. Synthesis and anti-enterovirus activity of new analogues of MDL-860
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