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  3. CYM5442 hydrochloride

CYM5442 hydrochloride 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 hydrochloride 对 S1P2,S1P3,S1P4 和 S1P5 无活性。CYM5442 hydrochloride 激活依赖 S1P1 的 p42/p44-MAPK 磷酸化。CYM5442 hydrochloride 具有视网膜神经保护作用,并可轻松穿过中枢神经系统。

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CYM5442 hydrochloride Chemical Structure

CYM5442 hydrochloride Chemical Structure

CAS No. : 1783987-80-3

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CYM5442 hydrochloride 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride 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 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 CYM-5442 in E121A S1P1 cells is concentration dependent, with a mean EC50 value of 134 nM[1].

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

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].

MCE 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)[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

445.94

Formula

C23H28ClN3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

CYM5442 hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CYM5442 hydrochloride
目录号:
HY-10968A
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