Icanbelimod S1p receptor agonist 1,99.95%

产品编号:Bellancom-101265| CAS NO:1514888-56-2| 分子式:C23H24FN3O3| 分子量:409.45

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-101265
500.00 杭州 北京(现货)
Bellancom-101265
2000.00 杭州 北京(现货)
Bellancom-101265
3500.00 杭州 北京(现货)
Bellancom-101265
11000.00 杭州 北京(现货)

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Icanbelimod S1p receptor agonist 1

产品介绍 Icanbelimod (S1p receptor agonist 1) 是一种有效的口服活性 S1P?receptor 激动剂,具有诱导 S1P1 内化的活性 (EC50=9.83 nM)。Icanbelimod 有潜力用于研究关节炎和 EAE (实验性自身免疫性脑炎) 的相关研究。Icanbelimod 是专利 WO2015039587A1 中的化合物 2。
生物活性

Icanbelimod (S1p receptor agonist 1) is a potent and orally active?S1P?receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.

体外研究
体内研究

Icanbelimod (oral administration; 0.01 mg/kg-1 mg/kg) at all dose is active, and only a dose of 0.01 mg/kg is required to observe a decrease in the number of peripheral blood lymphocytes by more than 50% and a decrease in the 1 mg/kg dose. Besides, this compound is lymphocyte-specific, which dose not significantly alter the number of peripheral monocytes and other white blood cells in SD rats.
Icanbelimod (oral administration; 3 mg/kg; 12 days) is has been proved to block lymphocyte efflux. In the development of type II collagen-induced arthritis in rat model, compound 2 is effective in inhibiting the development of joint swelling in arthritis and joint structure destruction.
Icanbelimod (oral administration; 0.3-1mg/kg; 30 days; once daily) inhibits the development of experimental autoimmune encephalitis (EAE) as a dose-dependent manner in mice model.

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

Animal Model: Lewis rats
Dosage: 3 mg/kg
Administration: Oral administration
Result: Decreased the severity score of arthritis in the four-legged rats.
Animal Model: Female C57BL/6 mice 
Dosage: 0.03, 0.1, and 1 mg/kg
Administration: Oral administration
Result: Decreased the severity score of EAE in MOG 35-55 induced mice.
体内研究

Icanbelimod (oral administration; 0.01 mg/kg-1 mg/kg) at all dose is active, and only a dose of 0.01 mg/kg is required to observe a decrease in the number of peripheral blood lymphocytes by more than 50% and a decrease in the 1 mg/kg dose. Besides, this compound is lymphocyte-specific, which dose not significantly alter the number of peripheral monocytes and other white blood cells in SD rats.
Icanbelimod (oral administration; 3 mg/kg; 12 days) is has been proved to block lymphocyte efflux. In the development of type II collagen-induced arthritis in rat model, compound 2 is effective in inhibiting the development of joint swelling in arthritis and joint structure destruction.
Icanbelimod (oral administration; 0.3-1mg/kg; 30 days; once daily) inhibits the development of experimental autoimmune encephalitis (EAE) as a dose-dependent manner in mice model.

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

Animal Model: Lewis rats
Dosage: 3 mg/kg
Administration: Oral administration
Result: Decreased the severity score of arthritis in the four-legged rats.
Animal Model: Female C57BL/6 mice 
Dosage: 0.03, 0.1, and 1 mg/kg
Administration: Oral administration
Result: Decreased the severity score of EAE in MOG 35-55 induced mice.
性状Solid
溶解性数据
In Vitro: 

DMSO : 6.8 mg/mL (16.61 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4423 mL 12.2115 mL 24.4230 mL
5 mM 0.4885 mL 2.4423 mL 4.8846 mL
10 mM 0.2442 mL 1.2212 mL 2.4423 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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