「同位素标记抑制剂」CAS:1202866-92-9|Mycophenolic acid-13C17
【产品介绍】:
生物活性:Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
IC50 & Target:Mycophenolic acid (MPA) is an immunosuppressant drug used to prevent rejection in organ transplantation. It inhibits an enzyme needed for the growth of T cells and B cells. Mycophenolic acid (MPA) did not block the initial phase of viral translation but did interfere with viral protein synthesis in the amplification phase. Quantitative RT-PCR demonstrated that MPA prevented the accumulation of viral positive- and negative-strand RNA as the infection proceeded. Mycophenolic acid (MPA) inhibits flavivirus infection by preventing synthesis and accumulation of viral RNA[1]. The effects of Mycophenolic acid (MPA) on DEN replication in monkey kidney (LLC-MK2) cells were examined. MPA (IC50=0.4+/-0.3 microM) inhibited DEN2 replication. Quantitative real-time RT-PCR of viral RNA and plaque assays of virions from DEN2-infected and Mycophenolic acid (MPA) (10 microM) -treated cells showed a fivefold increase in defective viral RNA production by cells treated with each drug. suggesting that one mode of antiviral action of MPA is by inhibition of inosine monophosphate dehydrogenase and thereby depletion of the intracellular GTP pool[2].
体外研究(In Vitro):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]。Mycophenolic acid 对多种 RNA 病毒具有抗病毒作用,包括流感、登革热病毒、寨卡病毒、轮状病毒、CCHFV 和汉坦病毒[2]。
IMPDH 是鸟苷核苷酸从头合成中的限速酶[3]。
Mycophenolic acid (0.01-1 μM; 72 小时) 对内皮细胞和成纤维细胞表现出优先的抗增殖活性。内皮细胞是对霉酚酸处理最敏感的细胞,其抗有丝分裂作用的 IC50<500 nM[3]。
Mycophenolic acid 在成纤维细胞中抑制细胞周期,但与内皮细胞相比表现出更好的 IC50 (<1 μM) 浓度。两种人类肿瘤细胞系 A549 非小细胞肺癌细胞和 PC3 前列腺癌细胞表现出中等敏感性,IC50 >1 μM。U87 胶质母细胞瘤细胞对高达 1 μM 的 MPA 处理具有抗性[3]。
Mycophenolic acid(0.05-2 μM;18 小时)表现出剂量依赖性下调 HDAC2 和 MYC,同时上调 NDRG1 水平[4]。
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Mycophenolic acid-13C17 相关抗体:
Phospho-IRF3 (Ser386) Antibody
IRF3 Antibody
分子量:337.21
Formula:13C17H20O6
CAS 号:1202866-92-9
非标记 CAS:24280-93-1
中文名称:霉酚酸-13C17
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
Data Sheet (537 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-220.
[Content Brief]
[2]. Sophie Domhan, et al. Molecular mechanisms of the antiangiogenic and antitumor effects of mycophenolic acid. Mol Cancer Ther. 2008 Jun;7(6):1656-68.
[Content Brief]
[3]. Stephen R Welch, et al. Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. Viruses. 2021 Jun 28;13(7):1255.
[Content Brief]