1429374-83-3
1429374-83-3 structure
- Name: Izuforant
- Chemical Name: Izuforant
- CAS Number: 1429374-83-3
- Molecular Formula: C12H12BrN7
- Molecular Weight: 334.17
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2022-09-01 17:03:27
- Modify Date: 2024-04-09 16:32:00
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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].
| Name | Izuforant |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
Human H4 Receptor:36 nM (IC50) h5-HT3R:9.1 μM (IC50) |
| In Vitro | 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: 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 |
| References |
[1]. Pil Su Ho, et al. Novel heterocyclic derivatives and their uses. WO2013048214A2. |
| Molecular Formula | C12H12BrN7 |
|---|---|
| Molecular Weight | 334.17 |