Rn-9893 is an effective compound that selectively antagonizes the transient receptor potential ion channel TRPV4. The IC50 values of RN-9893 on human, rat and mouse TRPV4 receptors were 420 nM, 660 nM and 320 nM, respectively. Rn-9893 showed no inhibition of TRPV1 at the concentration of 10 μM, the IC50 of TRPV3 was >, the IC50 of TRPV3 was 30 μM, and the IC50 of TRPM8 was about 30 μM. Rn-9893 showed good selectivity for 54 common biological targets.
| Molecular Weight | 500.49 |
| Formula | C21H23F3N4O5S |
| CAS Number | 1803003-68-0 |
| Solubility (25°C) | DMSO: 25 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.
[2] Zhi-Liang Wei, et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel
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