产品
编 号：F745112
分子式：C12H12BrN7
分子量：334.17
分子式：C12H12BrN7
分子量：334.17
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CAS No: 1429374-83-3
产品详情
生物活性：
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.
体内研究：
Izuforant (JW1601) (50 mg/kg; p.o.; once) decreases histamine-and substance P-induced itching in mice.Izuforant (100 mg/kg; p.o.; twice a day for 3 weeks) inhibits oxazolone-induced atopic dermatitis in mice.Animal Model:Female, ICR mice (8 weeks old)
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)
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)
Dosage:50 mg/kg for mice and 10 mg/kg for rats
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Pharmacokinetics parameter of Izuforant (Compound 24)Compound MouseRat
t1/2 (h)Cmax (μg/mL)AUCinf (μg?hr/mL)t1/2 (h)Cmax (μg/mL)AUCinf (μg?hr/mL)
Izuforant0.9618.8732.171.302.424.51
体外研究：
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.
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.
体内研究：
Izuforant (JW1601) (50 mg/kg; p.o.; once) decreases histamine-and substance P-induced itching in mice.Izuforant (100 mg/kg; p.o.; twice a day for 3 weeks) inhibits oxazolone-induced atopic dermatitis in mice.Animal Model:Female, ICR mice (8 weeks old)
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)
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)
Dosage:50 mg/kg for mice and 10 mg/kg for rats
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Pharmacokinetics parameter of Izuforant (Compound 24)Compound MouseRat
t1/2 (h)Cmax (μg/mL)AUCinf (μg?hr/mL)t1/2 (h)Cmax (μg/mL)AUCinf (μg?hr/mL)
Izuforant0.9618.8732.171.302.424.51
体外研究：
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.
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