1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Izuforant

Izuforant (Synonyms: JW1601)

Cat. No.: HY-147276
Handling Instructions

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.

For research use only. We do not sell to patients.

Izuforant Chemical Structure

Izuforant Chemical Structure

CAS No. : 1429374-83-3

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

334.17

Formula

C12H12BrN7

CAS No.
SMILES

CNC1CN(C2=NC3=NC=C(Br)C=C3N4C2=NN=C4)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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