熔点：
223-225°C
外观与性状：
黄色粉末
包装规格：
1g in glass bottle
产品简介：
一种重组PDE5的抑制剂，IC50:5.9μM。
Icariin is an inhibitor of human recombinant PDE5 with an IC50 value of 5.9 μM. It is a prenylated flavonol that has been shown to have anti-cancer and antioxidant activity. At a concentration of 1 x 107 mol/L, Icariin induces differentiation of cardiomyocytes and upregulates the expression of cardiac genes. At 20 μg/ml, Icariin increases the proliferation and differentiation of cultured human osteoblasts, which appears to be mediated in part by upregulating bone
溶解性：
溶于DMSO(50mg/mL)
储备液保存：
-80°C, 2 years
-20°C, 1 year
-20°C, 1 year
体内实验：
1、请依序添加每种溶剂： 0.5% CMC/saline water
Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic
2、请依序添加每种溶剂： 50% PEG300→50% saline
Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic
3、请依序添加每种溶剂： 10% DMSO→90% corn oil
Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.69 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。
4、请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% saline
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.07 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
5、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (3.07 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (3.07 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic
2、请依序添加每种溶剂： 50% PEG300→50% saline
Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic
3、请依序添加每种溶剂： 10% DMSO→90% corn oil
Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.69 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。
4、请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% saline
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.07 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
5、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (3.07 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (3.07 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
靶点：
PDE5：432 nM (IC50)
PDE4：73.5 μM (IC50)
PPARα
Autophagy
PDE4：73.5 μM (IC50)
PPARα
Autophagy
体外研究：
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. 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.
Icariin protects BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway.
Icariin protects BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway.
体内研究：
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. 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.
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
保存条件：
室温
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
