JNJ-55511118 is an AMPA receptor negative regulator containing transmembrane AMPA receptor regulatory protein γ8 (TARP-γ8). 1 It inhibits glutamate-induced calcium flux in HEK293F cells that were cotransfected with TARP-γ8 and GluA1o, GluA1i, GluA2i, GluA3o, or GluA4o (IC50s = 11.22, 12.3, 7.41, 38.02, and 15.85 nM, respectively).
| Molecular Weight | 328.67 |
| Formula | C14H8ClF3N2O2 |
| CAS Number | 2036081-86-2 |
| Solubility (25°C) | Soluble in DMSO |
| 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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