| Size | Price | |
|---|---|---|
| 100mg | ||
| 500mg |
| ln Vitro |
Numerous RNA viruses, such as the influenza virus, dengue virus, Zika virus, rotavirus, CCHFV, and hantavirus, are susceptible to the antiviral actions of mycophenolate sodium [1]. The enzyme that limits the pace of de novo guanosine nucleotide synthesis is called IMPDH [2]. Endothelial cells and fibroblasts are the primary targets of the selective antiproliferative effect of mycophenolic acid sodium (0.01-1 μM; 72 h). The most susceptible cells to mycophenolic acid therapy are endothelial cells, whose antimitotic IC50 is less than 500 nM[2]. While fibroblasts have a greater IC50 (<1 μM) than endothelial cells, they are nonetheless vulnerable to mycophenolic acid-induced cell cycle inhibition. A549 non-small cell lung cancer cells and PC3 prostate cancer cells, two human tumor cell lines, demonstrated considerable sensitivity with an IC50 > 1 μM. Up to 1 μM of mycophenolate sodium therapy does not affect U87 glioblastoma cells [2]. There is a dose-dependent down-regulation of HDAC2 and MYC and an up-regulation of NDRG1 when mycophenolic acid (0.05-2 μM; 18 hours) sodium is applied [2].
|
|---|---|
| ln Vivo |
By controlling the tumor microenvironment, mycophenolic acid (120 mg/kg; oral gavage; bid) sodium exhibits anti-tumor actions, notably inhibiting the formation of U87 tumors in BALB/c nude mice [2].
|
| Cell Assay |
Cell proliferation assay [2]
Cell Types: primary isolated human dermal microvascular endothelial cells (HDMVEC), fibroblasts, U87 glioblastoma cells, PC3 prostate cancer cells, A549 non-small cell lung cancer cells. Tested Concentrations: 0.01, 0.1, 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated preferential antiproliferative activity on HDMVEC and fibroblasts. U87 glioblastoma cells were resistant to treatment, whereas A549 non-small cell lung cancer and PC3 prostate cancer cells demonstrated intermediate sensitivity. Western Blot Analysis[2] Cell Types: HDMVEC Tested Concentrations: 0, 0.05, 0.1, 0.5, 1 and 2 μM Incubation Duration: 18 hrs (hours) Experimental Results: Shows dose-dependent regulation of HDAC2, MYC and NDRG1. |
| Animal Protocol |
Animal/Disease Models: Athymic 8weeks old, 20 g BALB/c nu/nu (nude) mice with mycophenolic acid-resistant human U87 tumor model [2]
Doses: 120 mg/kg MMF (mycophenolate mofetil prodrug) Mode of Route of Administration: po (oral gavage); bid Experimental Results: Compared with control mice, MMF (mycophenolate mofetil prodrug) Dramatically inhibited tumor growth in MMF-treated mice (approximately 14 days after tumor implantation) 70%). Microvessel density (CD31 staining) and pericyte coverage measured by α-smooth muscle actin staining were Dramatically diminished in MMF-treated tumors compared with control tumors (44% and 78%, respectively). |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Information from 3 patients on the excretion of mycophenolate into milk is inconsistent. A few infants have reportedly been breastfed during mycophenolate therapy, with no adverse effects reported. Because little information is available on the use of mycophenolate during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants The National Transplantation Pregnancy Registry (renamed Transplant Pregnancy Registry International) collected information on 6 mothers (5 kidney and 2 heart transplants) who breastfed 7 infants while taking a mycophenolate product. The maximum time that any of the infants was breastfed was 14 months. None of the infants had any reported adverse reactions. Another case series from the Transplant Pregnancy Registry International reported women who received heart transplants reported that 3 women breastfed their infants while taking mycophenolate. Durations of breastfeeding and infant outcomes were not reported. It is possible that some of these women were the same as those in the case series above. In case series of 77 patients from the UK who received either a liver or cardiothoracic transplant, 9 took mycophenolate mofetil throughout pregnancy. Overall, 60% breastfed their infants, although the exact number who breastfed with mycophenolate or their outcomes were not reported. An Australian case series reported 3 women with heart transplants who had a total of 5 infants, all of whom were breastfed (extent not stated). Two of the women took mycophenolate mofetil postpartum, one in a dosage of 720 mg twice daily and the other woman in a dosage of 1 gram twice daily. No adverse infant effects were reported up to the times of hospital discharge. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
Mycophenolate sodium is an organic sodium salt that is the sodium salt of mycophenolic acid. An immunosuppressant, it is widely used to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases. It has a role as an EC 1.1.1.205 (IMP dehydrogenase) inhibitor and an immunosuppressive agent. It contains a mycophenolate.
Mycophenolate Sodium is the sodium salt form of mycophenolic acid (MPA), with immunosuppressing activity. In vivo, the active molecule MPA reversibly inhibits inosine monophosphate dehydrogenase (IMPDH) which is needed for guanine monophosphate synthesis and stops the proliferation of B and T lymphocytes. Relative to other cell types, lypmocytes are highly dependent on salvage and de novo synthesis of guanine nucleotides, thus making these cells prone to MPA cytotoxicity. Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION. See also: Mycophenolic Acid (has active moiety). |
| Molecular Formula |
C17H19O6-.NA+
|
|---|---|
| Molecular Weight |
342.31896
|
| Exact Mass |
343.116
|
| CAS # |
37415-62-6
|
| Related CAS # |
Mycophenolic acid;24280-93-1
|
| PubChem CID |
23665584
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.29 g/cm3
|
| Boiling Point |
611.6ºC at 760 mmHg
|
| Flash Point |
225.8ºC
|
| LogP |
2.733
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
24
|
| Complexity |
492
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[Na+].O=C(CC/C(=C/CC1=C(OC)C(C)=C2COC(=O)C2=C1O)/C)[O-]
|
| InChi Key |
DOZYTHNHLLSNIK-JOKMOOFLSA-M
|
| InChi Code |
InChI=1S/C17H20O6.Na/c1-9(5-7-13(18)19)4-6-11-15(20)14-12(8-23-17(14)21)10(2)16(11)22-3;/h4,20H,5-8H2,1-3H3,(H,18,19);/q;+1/p-1/b9-4+;
|
| Chemical Name |
sodium;(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1H-2-benzofuran-5-yl)-4-methylhex-4-enoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9212 mL | 14.6062 mL | 29.2124 mL | |
| 5 mM | 0.5842 mL | 2.9212 mL | 5.8425 mL | |
| 10 mM | 0.2921 mL | 1.4606 mL | 2.9212 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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