Izuforant (JW1601) (Compound 24) has potent anti-inflammatory and anti-pruritic activities. Izuforant has a binding affinity for human serotonin 3 receptor (h5-HT3R) with an IC50 value of 9.1 μM. Izuforant is also an orally active antagonist of histamine H4 receptor (H4R) with an IC50 value of 36 nM against human H4R [1] [2].

Izuforant (JW1601) (Compound 24) shows metabolic stability with CL h,int values of 3.05 and 1.33 mL/min/mg in mouse and human, respectively [1].

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 t 1/2 (h) C max (μg/mL) AUC inf (μg hr/mL) t 1/2 (h) C max (μg/mL) AUC inf (μg hr/mL) Izuforant 0.96 18.87 32.17 1.30 2.42 4.51