JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
 |
Source | J Neurophysiol (2012). Figure 1. JTE 013 |
| Method | RT-PCR | |
| Cell Lines | sensory neurons | |
| Concentrations | 100 nM | |
| Incubation Time | 15-min | |
| Results | The number of APs at each time point was then normalized to the respective control values, and this analysis demonstrated that JTE-013 produced a rapid and significant increase in excitability in 70% of the sensory neurons compared with their control values |
| Molecular Weight | 408.29 |
| Formula | C17H19Cl2N7O |
| CAS Number | 383150-41-2 |
| Solubility (25°C) | DMSO 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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