| Identification | Back Directory | [Name]
Toreforant | [CAS]
952494-46-1 | [Synonyms]
Toreforant JNJ-38518168 5-(4,6-dimethyl-1H-benzimidazol-2-yl)-4-methyl-N-[3-(1-methylpiperidin-4-yl)propyl]pyrimidin-2-amine | [Molecular Formula]
C23H32N6 | [MDL Number]
MFCD28502108 | [MOL File]
952494-46-1.mol | [Molecular Weight]
392.54 |
| Chemical Properties | Back Directory | [Boiling point ]
611.2±65.0 °C(Predicted) | [density ]
1.148±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
11.15±0.30(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Toreforant is a histamine H4 receptor antagonists. | [in vivo]
The animals treated with 100 mg/kg toreforant have reduced disease severity scores. The reduction in scores is similar to JNJ 28307474. A model of histamine-induced scratching in CD-1 mice (n=5 per group) is used to judge the anti-pruritic effects of Toreforant. Unlike other H4R antagonists, Toreforant is not efficacious in reducing histamine-mediated pruritus. After oral administration to rats, Toreforant-derived radioactivity is widely distributed into tissues; however, it is not quantifiable in cerebellum, cerebrum, medulla, and spinal cord in either Long Evans or Sprague Dawley rats, suggesting that drug-derived radioactivity does not cross the blood-brain barrier. Neuropathic pain models in rats are conducted with Toreforant and an H4R antagonist that does cross the blood-brain barrier, JNJ 39758979. In a rat spinal nerve ligation model JNJ 39758979 was able to significantly attenuate the mechanical allodynia induced in the model, however Toreforant has no activity[1]. | [IC 50]
H4 receptor: 8.4±2.2 nM (IC50) | [storage]
Store at -20°C |
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