Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Izuforant (JW1601) (Compound 24) 具有有效的抗炎和止痒活性。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力,IC50值为 9.1 μM。它也是组胺 H4 受体 (H4R) 的口服活性拮抗剂,对人 H4R 的IC50值为 36 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | Izuforant (JW1601) (Compound 24) has potent anti-inflammatory and anti-pruritic activities. Izuforant has a binding affinity for human serotonin 3 receptor (h5-HT3R) with an IC50 value of 9.1 μM. Izuforant is also an orally active antagonist of histamine H4 receptor (H4R) with an IC50 value of 36 nM against human H4R [1] [2]. |
体外活性 | Izuforant (JW1601) (Compound 24) shows metabolic stability with CL h,int values of 3.05 and 1.33 mL/min/mg in mouse and human, respectively [1]. |
体内活性 | 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 t 1/2 (h) C max (μg/mL) AUC inf (μg hr/mL) t 1/2 (h) C max (μg/mL) AUC inf (μg hr/mL) Izuforant 0.96 18.87 32.17 1.30 2.42 4.51 |
分子量 | 334.17 |
分子式 | C12H12BrN7 |
CAS No. | 1429374-83-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Izuforant 1429374-83-3 Inhibitor inhibitor inhibit