NXY-059 is a free radical-trapping neuroprotectant that has been reported to reduce infarct size and preserve brain function in experimental models of acute ischemic stroke. NXY-059-treated animals significantly reduced the loss of hemispheric tissue compared to brain-injured controls (43.0 +/- 11 mm3 versus 74.4 +/- 19 mm3, respectively; p < 0.01). NXY-059 significantly attenuated the loss of injured brain tissue and improved cognitive outcome, suggesting a major role for ROS in the pathophysiology of TBI. NXY-059 is now under the Phase 2 clinical trial in patients with prelapsed or refractory multiple myeloma.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | transient focal cerebral ischemia in the rat model |
| Formulation | normal saline |
| Dosages | 0.3, 3 or 30 mg/kg |
| Administration | i.v. |
| Molecular Weight | 381.33 |
| Formula | C11H13NNa2O7S2 |
| CAS Number | 168021-79-2 |
| Solubility (25°C) | DMSO ≥60 mg/mL Water ≥60 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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