Name | mycophenolate sodium |
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Synonyms |
mycophenolicmonosodiumsalt
MYCOPHENOLATE SODIUM Mycophenolic acid monosodium salt sodiummycophenolate mycophenolicacidmonosodiumsalt |
Description | Mycophenolic acid sodium is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid sodium is an immunosuppressive agent. Antiangiogenic and antitumor effects[1][2]. |
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Related Catalog | |
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 the de novo synthesis 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 cell lung cancer cells and PC3 prostate cancer cells show intermediate sensitivity with 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. |
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/c nu/nu mice 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). |
References |
Density | 1.29 g/cm3 |
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Boiling Point | 611.6ºC at 760 mmHg |
Molecular Formula | C17H20NaO6+ |
Molecular Weight | 343.32700 |
Flash Point | 225.8ºC |
Exact Mass | 343.11600 |
PSA | 93.06000 |
LogP | 2.73320 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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RIDADR | UN 2811 6.1 / PGIII |
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