受注:045-509-1970 |
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Synonyms | BAY38-9456 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H32N6O4S.HCl.3H2O |
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分子量 | 579.11 | CAS No. | 330808-88-3 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (172.67 mM) | |
Ethanol | 100 mg/mL (172.67 mM) | |||
Water | 10 mg/mL (17.26 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. |
製品説明 | Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. |
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in vitro | Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. [1] Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. [2] Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle. [3] |
in vivo | Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. [1] Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. [2] Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. [4] Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening. [5] |
Data from [Data independently produced by , , Cancer Lett, 2016, 378(1):38-50.]
Data from [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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。