Mycophenolic acid sodium 是一种有效的非竞争性肌苷单磷酸脱氢酶 (IMPDH) 抑制剂，EC50为 0.24 μM。Mycophenolic acid sodium 对多种 RNA 病毒具有抗病毒作用，包括流感 (influenza)。Mycophenolic acid sodium 是一种免疫抑制剂。具有抗血管生成和抗肿瘤作用。
| 生物活性 | Mycophenolic acid sodium is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with anEC50of 0.24 μM. Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses includinginfluenza. Mycophenolic acid sodium is an immunosuppressive agent. Antiangiogenic and antitumor effects[1][2]. |
| IC50& Target | Human Endogenous Metabolite |
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体外研究
(In Vitro) | Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses including influenza, dengue virus, Zika virus, rotavirus, CCHFV, and hantavirus[1].
IMPDH is the rate-limiting enzyme in thede novosynthesis of guanosine nucleotides[2].
Mycophenolic acid (0.01-1 μM; 72 hours) sodium exhibits preferential antiproliferative activity against the endothelial cells and fibroblasts. Endothelial cells are most sensitive cells to Mycophenolic acid treatment with an IC50<500 nm for antimitotic effects[2].
Fibroblasts are also prone to Mycophenolic acid-induced cell cycle inhibition but exhibit a higher IC50(<1 μm) compared with endothelial cells. the two human tumor cell lines a549 non-small lung cancer cells and pc3 prostate show intermediate sensitivity an ic50>1 μM. U87 glioblastoma cells are resistant against Mycophenolic acid sodium treatment up to 1 μM[2].
Mycophenolic acid (0.05-2 μM; 18 hours) sodium exhibits a dose-dependent down-regulation of HDAC2 and MYC, whereas up-regulates NDRG1[2].
Cell Proliferation Assay[2] | Cell Line: | Primary isolated human dermal microvascular endothelial cells (HDMVEC) , fibroblasts, U87 glioblastoma cells, PC3 prostate cancer cells, A549 non-small cell lung cancer cells. | | Concentration: | 0.01, 0.1, 1 μM | | Incubation Time: | 72 hours | | Result: | Exhibited preferential antiproliferative activity against HDMVEC and fibroblasts. Whereas U87 glioblastoma cells were resistant to treatment, A549 non-small cell lung cancer and PC3 prostate cancer cells showed intermediate sensitivity. |
Western Blot Analysis[2] | Cell Line: | HDMVEC | | Concentration: | 0, 0.05, 0.1, 0.5, 1, and 2 μM | | Incubation Time: | 18 hours | | Result: | Showed a dose-dependent regulation of HDAC2, MYC, and NDRG1. |
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体内研究
(In Vivo) | Mycophenolic acid (120 mg/kg; oral gavage; b.i.d.) sodium exerts its antitumor effects via modulation of the tumor microenvironment, U87 tumor growth is markedly inhibited in vivo in BALB/c nude mice[2].
| Animal Model: | Athymic 8-week-old, 20 g BALB/cnu/numice bearing Mycophenolic acid-resistant human U87 tumor model[2] | | Dosage: | 120 mg/kg MMF (the morpholinoethyl ester prodrug of Mycophenolic acid) | | Administration: | Oral gavage; b.i.d. | | Result: | MMF (the morpholinoethyl ester prodrug of Mycophenolic acid) significantly inhibited tumor growth (~70% after day 14 after tumor implantation) in MMF-treated versus control mice.
Microvessel density (CD31 staining) and pericyte coverage determined by α-smooth muscle actin staining were markedly reduced in MMF-treated versus control tumors (44% and 78%, respectively). |
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| 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. |
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