|5-羟基-2-(4-甲氧基苯基)-8-(3-甲基丁-2-烯-1-基)-7-(((2S,3R,4S,5S,6R)-3,4,5-三羟基-6-(羟甲基)四氢-2H-吡喃-2-基)氧基)-3-(((2S,3R,4R,5R,6S)-3,4,5-三羟基-6-甲基四氢-2H-吡喃-2-基)氧基)-4H-苯并吡喃-4-酮|CsnPharm

CAS No.: 489-32-7

淫羊藿苷 Catalog No. CSN19464

Synonyms: 淫羊藿甙;Ieariline;淫羊藿苷

Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold selective for PDE5 than PDE4 and exhibits multiple biological properties, including anti-inflammatory, neuroregulatory and neuroprotective activities. It is a major constituent of flavonoids from the Chinese medicinal herb Epimedium brevicornum..

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生物活性

描述Icariin is a flavonol glycoside. It inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator^[3]. Icariin was injected in a dose of 50 mg/kg, and significantly reduced paw swelling in carrageenan-injected animals. It also ameliorated carrageenan-induced paw histopathological alterations. Icariin significantly increased paw enzymatic and non-enzymatic antioxidants. It decreased paw lipid peroxidation. Icariin decreased paw levels of inflammatory cytokines and NF-kB^[4]. Icariin can prevent the production of amyloid β (1-42) and inhibit the expression of amyloid precursor protein (APP) and β-site APP cleaving enzyme 1 (BACE-1) in animal models of Alzheimer's disease (AD). Icariin also prevents the neurotoxicity induced by hydrogen peroxide (H2O2), endoplasmic reticulum (ER) stress, ibotenic acid, and homocysteine^[5]. Icariin selectively inhibited proliferation and triggered apoptosis in breast cancer cells in a concentration- and time-dependent manner, but exhibited little cytotoxicity in normal breast cells. Moreover, icariin induced cell apoptosis via a mitochondria-mediated pathway, as indicated by the upregulated ratio of Bax/Bcl-2 and reactive oxygen species induction. Importantly, icariin impaired the activation of the NF-κB/EMT pathway, as evidenced by upregulation of SIRT6, resulting in inhibition of migration and invasion of breast cancer cells^[6]. Icariin protects BMSCs (bone marrow-derived mesenchymal stem cells) against OGD (oxygen, glucose and serum deprivation)-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02931305	Osteoporosis ... more >>Cardiovascular Disease Collapse <<	Phase 1	Unknown	October 2017	Singapore ... more >> Investigational Medicine Unit, National University Health System Recruiting Singapore, Singapore, 117599 Contact: Pei Ling Tan 6601 2534 angelia_pei_ling_tan@nuhs.edu.sg Collapse <<
NCT01979133	Bipolar Disorder ... more >> Substance Use Disorder Collapse <<	Phase 3	Completed	-	United States, Texas ... more >> The University of Texas Southwestern Medical Center Dallas, Texas, United States, 75390-8849 Collapse <<
NCT02112123	the Pharmacokinetic Profile of... more >> Icariin in Humans Collapse <<	Phase 1	Completed	-	United States, Texas ... more >> UT Southwestern Medical Center Dallas, Texas, United States, 75390 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4778 mL
- 7.3892 mL
- 14.7784 mL
- 5 mM
- 0.2956 mL
- 1.4778 mL
- 2.9557 mL
- 10 mM
- 0.1478 mL
- 0.7389 mL
- 1.4778 mL

技术信息

CAS号

489-32-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H40O15

运输

蓝冰

分子量

676.66

别名

淫羊藿甙;Ieariline;淫羊藿苷

溶解度

DMSO	49.0 mg/mL (72.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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