S1p receptor agonist 1

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1514888-56-2

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)。S1p receptor agonist 1 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。S1p receptor agonist 1 是专利 WO2015039587A1 中的化合物 2。

生物活性

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

IC₅₀& Target

EC50: 9.83 nM (S1P1 internalization)^[1]

体内研究
(In Vivo)

S1p receptor agonist 1 (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^[1].
S1p receptor agonist 1 (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^[1].
S1p receptor agonist 1 (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^[1].

Animal Model:	Lewis rats^[1]
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^[1]
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.

分子量

409.45

性状

Solid

Formula

C₂₃H₂₄FN₃O₃

CAS 号

1514888-56-2

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。