CYM5442|cas:1094042-01-9|西域试剂

CYM5442,98.83%

产品编号：Bellancom-10968| CAS NO：1094042-01-9| 分子式：C₂₃H₂₇N₃O₄| 分子量：409.48

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货号	价格	库存与货期
Bellancom-10968	￥1200.00	杭州北京（现货）
Bellancom-10968	￥1920.00	杭州北京（现货）
Bellancom-10968	￥6750.00	杭州北京（现货）
Bellancom-10968	￥10500.00	杭州北京（现货）

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CYM5442

产品介绍

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 active sphingosine 1-phosphate (S1P1) receptor agonist with an EC₅₀ of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS).

体外研究

CYM5442 (0.5 µM; 0-60 minutes; HEK293 cells) treatment stimulates S1P1 phosphorylation in a time-dependent manner in P32-orthophosphate labeled cells.
CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation in CHO-K1 cells transfected with S1P1 with an EC₅₀ of 46 nM. The R120 for alanine (R120A) mutant is still able to maintain p42/p44-MAPK activity when incubated with CYM5442 (EC₅₀ of 67 nM). Activation of p42/p44-MAPK by CYM5442 in E121A S1P1 cells is concentration dependent, with a mean EC₅₀ value of 134 nM.

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

Western Blot Analysis

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.

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

Animal Model:	Adult male albino Wistar rats (8-10 weeks old; 180-230 g) infected ocular endothelin-1 (ET-1)
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.

体内研究

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

Animal Model:	Adult male albino Wistar rats (8-10 weeks old; 180-230 g) infected ocular endothelin-1 (ET-1)
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.

体内研究

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

Animal Model:	Adult male albino Wistar rats (8-10 weeks old; 180-230 g) infected ocular endothelin-1 (ET-1)
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.

性状

Solid

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°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