Uses
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].
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: | Female, ICR mice (8 weeks old)[1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral administration, once |
| Result: | Decreased histamine-and substance P-induced itching. |
| Animal Model: | Female, Balb/c mice (6 weeks old, 20±3 g)[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral administration, twice a day for 3 weeks |
| Result: | Inhibited oxazolone-induced atopic dermatitis (51.2% inhibition). |
| Animal Model: | ICR mouse (20~30 g) and SD rat (200~300 g)[1] |
| Dosage: | 50 mg/kg for mice and 10 mg/kg for rats |
| Administration: | Oral administration (Pharmacokinetic Analysis) |
| Result: | Pharmacokinetics parameter of Izuforant (Compound 24)[1]
| Compound | | Mouse | | | | Rat | | | t1/2 (h) | Cmax (μg/mL) | AUCinf (μg?hr/mL) | | t1/2 (h) | Cmax (μg/mL) | AUCinf (μg?hr/mL) | | Izuforant | 0.96 | 18.87 | 32.17 | | 1.30 | 2.42 | 4.51 |
|
IC 50
Human H4 Receptor: 36 nM (IC50); h5-HT3R: 9.1 μM (IC50)
References
[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. DOI:10.4110/in.2018.18.e42
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