Mycophenolic acid [24280-93-1]

Référence HY-B0421-500mg

Conditionnement : 500mg

Marque : MedChemExpress

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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.

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Mycophenolic acid Chemical Structure

CAS No. : 24280-93-1

* Veuillez sélectionner la quantité avant d'ajouter des articles.

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  • J Agric Food Chem. 2023 Dec 28.  [Abstract]
  • Viruses. 2021 Jun 28;13(7):1255.  [Abstract]
  • Bone. 2022 Dec 21;168:116648.  [Abstract]
  • PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681.   [Abstract]
  • Curr Res Virol Sci. 2022;3:100019.  [Abstract]
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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.

Microbial Metabolite

 

Human Endogenous Metabolite

 

In Vitro

Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza, dengue virus, Zika virus, rotavirus, CCHFV, and hantavirus.
IMPDH is the rate-limiting enzyme in the de novo synthesis of guanosine nucleotides.
Mycophenolic acid (0.01-1 μM; 72 hours) 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.
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 MPA treatment up to 1 μM.
Mycophenolic acid (0.05-2 μM; 18 hours) exhibits a dose-dependent down-regulation of HDAC2 and MYC, whereas up-regulates NDRG1.

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

Cell Proliferation Assay

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

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 exerts its antitumor effects via modulation of the tumor microenvironment, U87 tumor growth is markedly inhibited in vivo in BALB/c nude mice.

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

Animal Model: Athymic 8-week-old, 20 g BALB/c nu/nu mice bearing Mycophenolic acid-resistant human U87 tumor model
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).

320.34

C17H20O6

24280-93-1

Solid

White to off-white

O=C(O)CC/C(C)=C/CC1=C(O)C2=C(COC2=O)C(C)=C1OC

  • Ketones, Aldehydes, Acids

several species of Penicillium

Room temperature in continental US; may vary elsewhere.

In Vitro: 

DMSO : ≥ 100 mg/mL (312.17 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1217 mL 15.6084 mL 31.2168 mL
5 mM 0.6243 mL 3.1217 mL 6.2434 mL
10 mM 0.3122 mL 1.5608 mL 3.1217 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  Corn Oil

    Solubility: 33.33 mg/mL (104.05 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
  • [1]. 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]

    [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]

  • [1]. 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.

    [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.

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  • Apoptosis Anti-infection Metabolic Enzyme/Protease
  • Dengue virus Apoptosis Bacterial Fungal Endogenous Metabolite Antibiotic Flavivirus
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