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Toreforant

Cat. No. M40966
Toreforant Structure
Synonym:

JNJ-38518168

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Biological Activity

Toreforant is an orally active histamine H4 receptor antagonist that may be used in studies related to psoriasis.

Chemical Information
Molecular Weight 392.54
Formula C23H32N6
CAS Number 952494-46-1
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] David L Boyle et al. Inflamm Res. Toreforant, an orally active histamine H4-receptor antagonist, in patients with active rheumatoid arthritis despite methotrexate: mechanism of action results from a phase 2, multicenter, randomized, double-blind, placebo-controlled synovial biopsy study

[2] Ellen Frankel et al. J Drugs Dermatol. Efficacy and Safety of Toreforant, a Selective Histamine H4 Receptor Antagonist, for the Treatment of Moderate-to-Severe Plaque Psoriasis: Results from a Phase 2 Multicenter, Randomized, Double-blind, Placebo-controlled Trial

[3] Alexa P Kollmeier et al. Ann Allergy Asthma Immunol. A phase 2a study of toreforant, a histamine H4 receptor antagonist, in eosinophilic asthma

[4] Robin L Thurmond et al. Handb Exp Pharmacol. Clinical Development of Histamine H4 Receptor Antagonists

[5] Robin L Thurmond et al. J Rheumatol. Toreforant, A Histamine H4 Receptor Antagonist, in Patients with Active Rheumatoid Arthritis Despite Methotrexate Therapy: Results of 2 Phase II Studies

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Keywords: Toreforant, JNJ-38518168 supplier, Histamine Receptor, inhibitors, activators


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