Bioactivity | Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies[1][2]. |
Invitro | Izuforant (JW1601) (Compound 24) shows metabolic stability with CLh,int values of 3.05 and 1.33 mL/min/mg in mouse and human, respectively[1]. |
In Vivo | Izuforant (JW1601) (50 mg/kg; p.o.; once) decreases histamine-and substance P-induced itching in mice[1].Izuforant (100 mg/kg; p.o.; twice a day for 3 weeks) inhibits oxazolone-induced atopic dermatitis in mice[1]. Animal Model: |
Name | Izuforant |
CAS | 1429374-83-3 |
Formula | C12H12BrN7 |
Molar Mass | 334.17 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Pil Su Ho, et al. Novel heterocyclic derivatives and their uses. WO2013048214A2. [2]. Jin M, et al. From Bench to Clinic: the Potential of Therapeutic Targeting of the IL-22 Signaling Pathway in Atopic Dermatitis. Immune Netw. 2018 Dec 19;18(6):e42. |