Mycophenolic acid (Synonyms:霉酚酸; Mycophenolate)
目录号 : KM16451 CAS No. : 24280-93-1 纯度 : 98%

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。

规格 价格 是否有货 数量
100mg
In-stock
500mg
In-stock
1g
In-stock
5g 询价 In-stock
10g 询价 In-stock

Other Forms of Rapamycin:

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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.

体外研究

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.

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. 
体内研究

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.

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).
分子式
C17H20O6
分子量
320.34
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。

  • 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。

  • 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。

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