Mycophenolic acid(Synonyms: 霉酚酸; Mycophenolate)

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Mycophenolic acid (Synonyms: 霉酚酸; Mycophenolate) 纯度: 99.87%

Mycophenolic acid 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 对多种 RNA 病毒具有抗病毒作用，包括流感 (influenza)。Mycophenolic acid 是一种免疫抑制剂。具有抗血管生成和抗肿瘤作用。

Mycophenolic acid(Synonyms: 霉酚酸; Mycophenolate)

Mycophenolic acid Chemical Structure

CAS No. : 24280-93-1

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10 mM * 1 mL in DMSO ￥605 In-stock
100 mg ￥550 In-stock
500 mg ￥1100 In-stock
1 g ￥1500 In-stock
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生物活性

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[1][2].

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Mycophenolic acid 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) 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 MPA treatment up to 1 μM[2].
Mycophenolic acid (0.05-2 μM; 18 hours) exhibits a dose-dependent down-regulation of HDAC2 and MYC, whereas up-regulates NDRG1[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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. 

体内研究
(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[2].

上海金畔生物科技有限公司 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[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).

Clinical Trial

分子量

320.34

Formula

C17H20O6
CAS 号

24280-93-1
中文名称

霉酚酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (312.17 mM)

H2O : 0.1 mg/mL (0.31 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    此方案可获得 ≥ 2.5 mg/mL (7.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

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

    此方案可获得 ≥ 2.5 mg/mL (7.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 2.5 mg/mL (7.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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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