CYM5442

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CYM5442

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:

1094042-01-9

CYM5442 是一种有效的，高选择性和口服活性的鞘氨醇 1-磷酸 (S1P1) 受体激动剂，EC₅₀为 1.35 nM。CYM5442 对 S1P2，S1P3，S1P4 和 S1P5 无活性。CYM5442 激活依赖S1P1的 p42/p44-MAPK 磷酸化。CYM5442 具有视网膜神经保护作用，并可轻松穿过中枢神经系统。

生物活性

CYM5442 is a potent, highly-selective and orally activesphingosine 1-phosphate (S1P1) receptoragonist with anEC₅₀of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activatesS1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS)^[1]^[2].

IC₅₀& Target

EC50: 1.35 nM (Sphingosine 1-phosphate (S1P1) receptor)^[1]

体外研究
(In Vitro)

CYM5442 (0.5 μM; 0-60 minutes; HEK293 cells) treatment stimulates S1P1 phosphorylation in a time-dependent manner in P32-orthophosphate labeled cells^[1].
CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation in CHO-K1 cells transfected with S1P1 with an EC₅₀of 46 nM. The R120 for alanine (R120A) mutant is still able to maintain p42/p44-MAPK activity when incubated with CYM5442 (EC₅₀of 67 nM). Activation of p42/p44-MAPK by CYM5442 in E121A S1P1 cells is concentration dependent, with a mean EC₅₀value of 134 nM^[1].

Western Blot Analysis^[1]

Cell Line:	HEK293 cells stably expressing S1P1 fused to GFP on the carboxy-terminus
Concentration:	0.5 μM
Incubation Time:	0 minutes, 2 minutes, 5 minutes, 10 minutes, 30 minutes, 60 minutes
Result:	Stimulated S1P1 phosphorylation in a time-dependent manner.

体内研究
(In Vivo)

CYM5442 (1 mg/kg; intraperitoneal injection; daily; for 5 days; adult male albino Wistar rats) treatment shows preserved visual function of visual evoked potentials (VEP). Retinal nerve fiber layer (RNFL) is significantly thicker in the CYM treated-animals compared to the vehicle^[2].

Animal Model:	Adult male albino Wistar rats (8-10 weeks old; 180-230 g) infected ocular endothelin-1 (ET-1)^[2]
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; daily; for 5 days
Result:	Visual evoked potentials (VEP) showed preserved visual function. Showed significantly higher retinal ganglion cells (RGCs) numbers.

分子量

409.48

性状

Solid

Formula

C₂₃H₂₇N₃O₄

CAS 号

1094042-01-9

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 : 2.63 mg/mL(6.42 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.4421 mL	12.2106 mL	24.4212 mL
5 mM	0.4884 mL	2.4421 mL	4.8842 mL
10 mM	---	---	---

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。