Izuforant (JW1601) (Compound 24) 是一种具有口服活性的组胺 H4 受体 (H4R) 拮抗剂，对人 H4R 的IC50为 36 nM。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力，IC50为 9.1 μM。 Izuforant 具有较强的止痒和抗炎作用。
| 生物活性 | Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with anIC50of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with anIC50of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies[1][2]. |
| IC50& Target | Human H4Receptor 36 nM (IC50) | h5-HT3R 9.1 μM (IC50) |
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体外研究
(In Vitro) | Izuforant (JW1601) (Compound 24) shows metabolic stability with CLh,intvalues of 3.05 and 1.33 mL/min/mg in mouse and human, respectively[1].
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体内研究
(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(μgohr/mL) | | t1/2(h) | Cmax(μg/mL) | AUCinf(μgohr/mL) | | Izuforant | 0.96 | 18.87 | 32.17 | | 1.30 | 2.42 | 4.51 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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