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医薬品及び創薬化学品の専門商社

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化合物検索・調査依頼・データベース提供生理・薬理活性化合物/ポジコン

Icariin【別名:Ieariline】

HY-N0014構造式

CAS No.
489-32-7
製品コード
HY-N0014
サプライヤー
Medchemexpress
純度
>98%
Target
Phosphodiesterase (PDE);PPAR;Autophagy
参考納期(在庫有りの場合)
約5-10営業日

詳細情報

FormulaC33H40O15
M.W.676.66
PathwayMetabolic Enzyme/Protease;Cell Cycle/DNA Damage;Autophagy
SolubilityDMSO: ? 34 mg/mL
備考Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
IC50 & Target: IC50: 432 nM (PDE5), 73.50 μM (PDE4)[1]

PPARα[2]
In Vitro: Icariin is a cGMP-specific PDE5 inhibitor. The inhibitory effects of Icariin on PDE5 and PDE4 activities are investigated by the two-step radioisotope procedure with 3H-cGMP/ 3H-cAMP. The potency of selectivity of Icariin on PDE5 (PDE4/PDE5 of IC50) is 167.67 times[1]. Cell viability is measured in the present study to evaluate whether Icariin protect endothelial HUVECs from injuries induced by oxidized low-density lipoprotein (ox-LDL). The exposure of the cells to ox-LDL for 24 h significantly decreases the cell viability compared with control group (P<0.05). However, Icariin can inhibit cell injury induced by ox-LDL in a concentration-dependent manner, and has significant difference (P<0.05) compared with ox-LDL-simulated group[3].
In Vivo: Icariin is a PPARα activator, induces Cyp4a10 and Cyp4a14, and regulates the mRNA levels of lipid metabolism enzymes and proteins, including fatty acid binding protein, fatty acid oxidation in mitochondria and in peroxisome. Icariin is effective in the treatment of hyperlipidemia. To understand the effect of Icariin on lipid metabolism, effects of Icariin on PPARα and its target genes are investigated. Mice are treated orally with Icariin at doses of 0, 100, 200, and 400 mg/kg, or Clofibrate (500 mg/kg) for five days. Liver total RNA is isolated and the expressions of PPARα and lipid metabolism genes are examined. PPARα and its marker genes Cyp4a10 and Cyp4a14 are induced 2-4 fold by Icariin, and 4-8 fold by Clofibrate. The fatty acid (FA) binding and co-activator proteins Fabp1, Fabp4 and Acsl1 are increased 2-fold. The mRNAs of mitochondrial FA β-oxidation enzymes (Cpt1a, Acat1, Acad1 and Hmgcs2) are increased 2-3 fold. The mRNAs of proximal β-oxidation enzymes (Acox1, Ech1, and Ehhadh) are also increased by Icariin and Clofibrate. The expression of mRNAs for sterol regulatory element-binding factor-1 (Srebf1) and FA synthetase (Fasn) are unaltered by Icariin. The lipid lysis genes Lipe and Pnpla2 are increased by Icariin and Clofibrate[2]. Adult rats are treated orally with Icariin at doses of 0 (control), 50, 100, or 200 mg/kg body weight for 35 consecutive days. The results show that Icariin has virtually no effect on the body weight or organ coefficients of the testes or epididymides. However, 100 mg/kg Icariin significantly increases epididymal sperm counts. In addition, 50 and 100 mg/kg Icariin significantly increase testosterone levels. Furthermore, 100 mg/kg Icariin treatment also affects follicle stimulating hormone receptor (FSHR) and claudin-11 mRNA expression in Sertoli cells. Superoxide dismutase (SOD) activity and malondialdehyde (MDA) levels are measured in the testes; 50 and 100 mg/kg Icariin treatment improve antioxidative capacity, while 200 mg/kg Icariin treatment upregulates oxidative stress[4].
URLhttps://www.medchemexpress.com/Icariin.html

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10mM/1mL : 101,700
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100mg : 12,200
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200mg : 17,100
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