Body weight changes of both sexes are not related to KR-33493 in all doses. In rats administrated KR-33493 for 4 weeks, no test article-related changes in any treated groups of either sex are found in hematology, serum biochemistry, and urinalysis. In dogs administrated KR-33493 for 2 weeks, red blood cell count (RBC) value in males is significantly higher at the 1000 mg/kg/day dose than that of the control group (i.e., 6.96±0.323 vs. 6.12±0.418). However, the change of RBC is recovered after the end of the administration period. The dose-normalized AUClast is not significantly different between the groups, suggesting that KR-33493 is governed by linear kinetics
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | specific pathogen-free rats |
| Formulation | |
| Dosages | 50, 150, and 500 mg/kg/day |
| Administration | i.v. |
| Molecular Weight | 460.34 |
| Formula | C20H18BrN3O3S |
| CAS Number | 1021497-97-1 |
| Form | Solid |
| Solubility (25°C) | 31 mg/mL 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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