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

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。

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Izuforant Chemical Structure

Izuforant Chemical Structure

CAS No. : 1429374-83-3

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Izuforant 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

IC50 & Target

Human H4 Receptor

36 nM (IC50)

h5-HT3R

9.1 μM (IC50)

体外研究
(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.

Izuforant 相关抗体:
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].

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
分子量

334.17

Formula

C12H12BrN7
CAS 号
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.
纯度 & 产品资料
参考文献

Izuforant 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Izuforant1429374-83-3JW1601JW 1601JW-1601Histamine Receptoranti-pruriticanti-inflammatoryhuman serotonin 3 receptorh5-HT3RInhibitorinhibitorinhibit

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