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丹皮酚 /Paeonol {[allProObj[0].p_purity_real_show]}

货号:A173012 同义名: 2-羟基-4-甲氧基苯乙酮 / 2'-Hydroxy-4'-methoxyacetophenone;Peonol

Paeonol is a naturally occuring MAO inhibitor with IC50 values of 54.6 μM and 42.5 μM for MAO-A and MAO-B, respectively.

Paeonol 化学结构 CAS号:552-41-0
Paeonol 化学结构
CAS号:552-41-0
Paeonol 3D分子结构
CAS号:552-41-0
Paeonol 化学结构 CAS号:552-41-0
Paeonol 3D分子结构 CAS号:552-41-0
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Paeonol 纯度/质量文件 产品仅供科研

货号:A173012 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 MAO MAO-A MAO-B 其他靶点 纯度
Sennoside A ++

MAO, IC50: 17 μM

98%+
Glycyrrhizic acid ++++

MAO, IC50: 0.16 μM

80% HPLC
Rasagiline ++++

MAO-A, IC50: 412 nM

++++

MAO-B, IC50: 4.43 nM

99+%
Isatin ++

MAO, IC50: 15 μM

+

MAO-A, IC50: 58 μM

++

MAO-B, IC50: 14 μM

98%
Paeonol +

MAO-A, IC50: 54.6 μM

+

MAO-B, IC50: 42.5 μM

98%
Tranylcypromine hydrochloride +++

MAO-A, IC50: 11.5 μM

+++

MAO-B, IC50: 7 μM

97%
Moclobemide +++

MAO-A (5-HT), IC50: 6.1 μM

99%+
Pargyline HCl ++

MAO-A, Ki: 13 μM

+++

MAO-B, Ki: 0.5 μM

99%+
Safinamide ++++

MAO-B, IC50: 98 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Paeonol 生物活性

靶点
  • MAO-B

    MAO-B, IC50:42.5 μM

  • MAO-A

    MAO-A, IC50:54.6 μM

描述 Monoamine oxidase (MAO) is an important enzyme in the metabolism of a wide range of endogenous monoamine neurotrasmitters such as noradrenaline, dopamine, and serotonin (5-HT), and also catalyzes as well the removal of exogenous amines. Paeonol, originated from the traditional Chinese medicine, is a naturally occuring MAO inhibitor with IC50 values of 54.6 μM and 42.5 μM for MAO-A and MAO-B, respectively[7]. Paeonol dose- and time- dependently induced not only antiproliferation activity and apoptosis but also autophagy via blocking the Akt/mTOR pathway in A2780 and SKOV3 cells. In addition, combination treatment with Paeonol and an autophagy inhibitor (3-methyladenine and hydroxychloroquine) showed significant synergetic effects on inhibiting cell viability and promoting apoptosis in vitro and in the A2780 xenograft model, without severe side effects[8]. Paeonol at 50 and 100μM prevented IL-1β-induced inflammatory response by inhibiting numerous factors of osteoarthritis(OA), including IL-6, TNF-a, NOX2, PTGS2, NUCB2/nesfatin-1, ICAM-1, VCAM-1, MMP-3/13, degradation of type II collagen, and NF-kB activation through the rescue of IkBa in human primary chondrocytes[9].

Paeonol 动物研究

Dose Mice: 20 mg/kg[3] (i.p.); 20 mg/kg - 80 mg/kg[4] (p.o.) Rat: 2.5 mg/kg - 10 mg/kg[5] (i.v.); 30 mg/kg - 100 mg/kg[2] (i.p.); 100 mg/kg, 200 mg/kg[6] (p.o.)
Administration i.p., p.o., i.v.
Pharmacokinetics
Animal Rats[5]
Dose 5 mg/kg
Administration i.v.
Vd 394 ± 22.8 L/kg
A 11.17 ± 0.93 μg/ml
B 1.72 ± 0.18 μg/ml
AUC 114.8 ± 10.3 μg·min/ml
T1/2β 30.6 ± 1.70 min
CL 49.3 ± 1.85 ml/min/kg
α 0.26 ± 0.03 1/min
β 0.023 ± 0.002 1/min

Paeonol 参考文献

[1]Kong LD, Cheng CH, Tan RX. Inhibition of MAO A and B by some plant-derived alkaloids, phenols and anthraquinones. J Ethnopharmacol. 2004 Apr;91(2-3):351-5.

[2]Chou TC. Anti-inflammatory and analgesic effects of paeonol in carrageenan-evoked thermal hyperalgesia. Br J Pharmacol. 2003 Jul;139(6):1146-52.

[3]Lee H, Lee G, et al. Paeonol, a major compound of moutan cortex, attenuates Cisplatin-induced nephrotoxicity in mice. Evid Based Complement Alternat Med. 2013;2013:310989.

[4]Antidepressant-like Effect of Paeonol

[5]Tsai TH, Chou CJ, et al. Pharmacokinetics of paeonol after intravenous administration in rats. J Pharm Sci. 1994 Sep;83(9):1307-9.

[6]Ma L, Chuang CC, et al. Paeonol Protects Rat Heart by Improving Regional Blood Perfusion during No-Reflow. Front Physiol. 2016 Jul 21;7:298.

[7]Kong LD, Cheng CH, Tan RX. Inhibition of MAO A and B by some plant-derived alkaloids, phenols and anthraquinones. J Ethnopharmacol. 2004 Apr;91(2-3):351-5. doi: 10.1016/j.jep.2004.01.013. PMID: 15120460.

[8]Gao L, Wang Z, Lu D, Huang J, Liu J, Hong L. Paeonol induces cytoprotective autophagy via blocking the Akt/mTOR pathway in ovarian cancer cells. Cell Death Dis. 2019 Aug 13;10(8):609. doi: 10.1038/s41419-019-1849-x. PMID: 31406198; PMCID: PMC6690917.

[9]Wang Q, Xu X, Kang Z, Zhang Z, Li Y. Paeonol prevents IL-1β-induced inflammatory response and degradation of type II collagen in human primary chondrocytes. Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):2139-2145. doi: 10.1080/21691401.2019.1613418. PMID: 31146598.

Paeonol 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.02mL

1.20mL

0.60mL

30.09mL

6.02mL

3.01mL

60.18mL

12.04mL

6.02mL

Paeonol 技术信息

CAS号552-41-0
分子式C9H10O3
分子量 166.174
别名 2-羟基-4-甲氧基苯乙酮 ;2'-Hydroxy-4'-methoxyacetophenone;Peonol;NSC 401442
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 40 mg/mL(240.71 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 1 mg/mL(6.02 mM),配合低频超声助溶

无水乙醇: 45 mg/mL(270.8 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方
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