D-erythro-Sphingosine-¹³C₂,d₂  (Synonyms: Erythrosphingosine-¹³C₂,d₂; erythro-C18-Sphingosine-¹³C₂,d₂; trans-4-Sphingenine-¹³C₂,d₂)

D-erythro-Sphingosine-13C2,d2 is a deuterated labeled D-erythro-Sphingosine^[1]. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC₅₀ of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator^[2][3][4][5].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
p32-鞘氨醇激活的蛋白激酶对低浓度的 D-erythro-Sphingosine 有反应，在 2.5 μM 时观察到初始激活，在 10 -20 μM 时观察到峰值活性。该激酶显示出对 D-erythro-Sphingosine 相对于其他鞘氨醇立体异构体的适度特异性，并且对鞘氨醇的偏好优于对异氢鞘氨醇^[2]。D-erythro-Sphingosine 在体外抑制蛋白激酶 C^[3]。D-erythro-Sphingosine 已显示可抑制影响细胞调节和多种信号转导通路的蛋白激酶 C，并在多种哺乳动物细胞中表现出抗肿瘤启动子活性^[4]。

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

303.49

C₁₆¹³C₂H₃₅D₂NO₂

2692623-81-5

123-78-4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Cheng P, et al. Protein phosphatase 2A (PP2A) activation promotes axonal growth and recovery in the CNS. J Neurol Sci. 2015 Dec 15;359(1-2):48-56.  [Content Brief]

  [3]. Pushkareva MYu, et al. Regulation of sphingosine-activated protein kinases: selectivity of activation by sphingoid basesand inhibition by non-esterified fatty acids. Biochem J. 1993 Sep 15;294 ( Pt 3):699-703.  [Content Brief]

  [4]. Khan WA, et al. Protein kinase C and platelet inhibition by D-erythro-Sphingosine: comparison with N,N-dimethylsphingosine and commercial preparation. Biochem Biophys Res Commun. 1990 Oct 30;172(2):683-91.  [Content Brief]

  [5]. Pham VT, et al. A concise synthesis of a promising protein kinase C inhibitor: D-erythro-Sphingosine. Arch Pharm Res. 2007 Jan;30(1):22-7.  [Content Brief]