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别名 | BAY38-9456 | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C23H32N6O4S.HCl.3H2O |
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分子量 | 579.11 | CAS号 | 330808-88-3 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (172.67 mM) | |
Water | 100 mg/mL (172.67 mM) | |||
Ethanol | 18 mg/mL (31.08 mM) | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | Vardenafil HCl Trihydrate (BAY38-9456)是一种新型PDE抑制剂,作用于PDE5和PDE1,IC50分别为0.7和180 nM。 | ||
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靶点 |
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体外研究 | Vardenafil特异性抑制PDE5介导cGMP的水解,IC50是0.7 nM(6.6 nM)。Vardenafi在3 nM(10 nM)显著提高了SNP诱导的人小梁平滑肌的松驰。Vardenafi显著诱导乙酰胆碱和电刺激诱发的小梁平滑肌的放松。[1] Vardenafil(100 mM)增加大鼠海马cGMP的水平。[2] Vardenafil, tadalafil和Sildenafil竞争性抑制cGMP的水解磷酸二酯酶5(PDE5),从而促进血管平滑肌中的cGMP的积累和松弛。[3] | ||
体内研究 | Vardenafil在兔子体内剂量依赖性诱导静脉注射Nitroprusside钠盐引起的勃起反应。[1] Vardenafil(3 毫克/千克,口服)导致大鼠中对象识别能力的改变。[2] Vardenafil(30 mg / L,p.o.)同时增加大鼠中iNOS和增殖细胞核抗原表达(SM细胞的复制),伴随动态海绵体融合下降率和SM/胶原蛋白比例的正常化。[4] 在兔的心脏中,Vardenafil通过打开线粒体K(ATP)通道诱导缺血/再灌注损伤强大的预处理般的心脏保护作用。Vardenafil通过依赖于线粒体K(ATP)通道开放机制,防止再灌注损伤的心肌缺血。[5] |
数据来源于[Data independently produced by , , Cancer Lett, 2016, 378(1):38-50.]
数据来源于[Data independently produced by , , Oncotarget, 2017, 8(5):8574-8589]
Impaired Redox and Protein Homeostasis as Risk Factors and Therapeutic Targets in Toxin-Induced Biliary Atresia [ Gastroenterology, 2020, 159(3):1068-1084.e2] | PubMed: 32505743 |
Skeletal restoration by phosphodiesterase 5 inhibitors in osteopenic mice: Evidence of osteoanabolic and osteoangiogenic effects of the drugs. [ Bone, 2020, 10.1016/j.bone.2020.115305] | PubMed: 32126313 |
Evaluation of the combination of endothelin receptor antagonists (ERA) and phosphodiesterase-5 inhibitors for the treatment of pulmonary arterial hypertension (PAH) in pathologic human pulmonary arteries in an ex-vivo organ bath model [ Pulm Pharmacol Ther, 2020, 66:101985] | PubMed: 33359621 |
Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression. [ Cancers (Basel), 2019, 11(11)] | PubMed: 31698786 |
Effect of RAD51C expression on the chemosensitivity of Eμ-Myc p19Arf-/- cells and its clinical significance in breast cancer [ Oncol Lett, 2018, 15(5):6107-6114] | PubMed: 29731842 |
FOXM1 evokes 5-fluorouracil resistance in colorectal cancer depending on ABCC10. [Xie T, et al. Oncotarget, 2017, 8(5):8574-8589] | PubMed: 28051999 |
Phosphodiesterase Inhibitors Sildenafil and Vardenafil Reduce Zebrafish Rod Photoreceptor Outer Segment Shedding. [ Invest Ophthalmol Vis Sci, 2017, 58(13):5604-5615] | PubMed: 29094165 |
Phosphodiesterase 5/protein kinase G signal governs stemness of prostate cancer stem cells through Hippo pathway. [Liu N, et al. Cancer Lett, 2016, 378(1):38-50] | PubMed: 27179930 |
Repurposing FDA-approved drugs for anti-aging therapies. [ Biogerontology, 2016, 17(5-6):907-920] | PubMed: 27484416 |
Inhibition of phosphodiesterase 5 reduces bone mass by suppression of canonical Wnt signaling. [Gong Y, et al. Cell Death Dis, 2014, 5:e1544] | PubMed: 25429621 |
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