IMT1 is the first, specific and non-competitive inhibitor of human mitochondrial RNA polymerase (POLRMT). IMT1 induces conformational changes in POLRMT that block substrate binding and transcription in a dose-dependent manner in vitro. IMT1 reduced deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in significant depletion of cellular amino acid levels. IMT1 has the potential to be used in the study of mitochondrial transcription and other related diseases.
| Molecular Weight | 351.4 |
| Formula | C21H21NO4 |
| CAS Number | 2304621-31-4 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 40 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.
[3] Lauren Passby. Med Teach. Melanin matters: Ethnic diversity in dermatology textbooks
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