Tapinarof (WBI-1001) is a Frist in class aromatic hydrocarbon receptor (AhR) agonist with EC50 of 13 nM. Tapinarof reduced skin inflammation in mice. It can effectively inhibit inflammatory cytokines, regulate skin barrier protein expression and antioxidant activity.
| Molecular Weight | 254.32 |
| Formula | C17H18O2 |
| CAS Number | 79338-84-4 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage | 4°C, protect from light, dry, sealed |
| 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.
[1] Mark G Lebwohl, et al. N Engl J Med. Phase 3 Trials of Tapinarof Cream for Plaque Psoriasis
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