Gepotidacin (GSK2140944) is a novel, potentially first-in-class, orally active triazaacenaphthylene antibiotic and type II topoisomerase (Topo II) inhibitor.Gepotidacin can selectively inhibit bacterial DNA replication by acting on DNA gyrase (GyrA) and topoisomerase IV (ParC).
| Molecular Weight | 448.52 |
| Formula | C24H28N6O3 |
| CAS Number | 1075236-89-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 7.14 mg/mL |
| Storage | -20°C |
| 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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Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. |
| ICRF-196
ICRF-196 is an racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193. |
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