Jnj-39758979 is a selective, orally active, high-affinity histamine H4 receptor antagonist with Ki values of 12.5, 5.3 and 25 nM for human, mouse and monkey histamine H4 receptor, respectively. Jnj-39758979 antagonized histamine-induced cAMP inhibition with a pA2 of 7.9. Jnj-39758979 has good anti-inflammatory and antipruritic effects.
| Molecular Weight | 221.3 |
| Formula | C11H19N5 |
| CAS Number | 1046447-90-8 |
| Solubility (25°C) | DMSO ≥ 20 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.
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