| CAS NO: | 330808-88-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| Molecular Weight (MW) | 579.11 |
|---|---|
| Formula | C23H32N6O4S.HCl.3H2O |
| CAS No. | 330808-88-3 (HCl trihydrate); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 116 mg/mL (200.3 mM) |
| Water: 116 mg/mL (200.3 mM) | |
| Ethanol: 20 mg/mL (34.53 mM) | |
| Other info | Chemical Name: 2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one dihydrochloride trihydrate InChi Key: NEAUGLIJDBPHAY-UHFFFAOYSA-N SMILES Code: O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.[H]Cl.[H]Cl.[H]O[H].[H]O[H].[H]O[H] |
| Synonyms | BAY38-9456; BAY 38-9456; BAY-38-9456; trade names: Levitra; Staxyn; Vivanza; Vardenafil hydrochloride trihydrate; Vardenafil HCl; Levitra; Staxyn; Vivanza |
| In Vitro | In vitro activity: 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. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle. Kinase Assay: Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM. Relative to PDE5, the ratios of the IC50 for PDE1 were 257 (60), for PDE6 16 (7.4). Cell Assay: Vardenafil significantly enhanced the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. |
|---|---|
| In Vivo | Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. 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. 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 |
| Animal model | Rabbit |
| Formulation & Dosage | 3 mg/kg, p.o. (rabbit) |
| References | Int J Impot Res. 2001 Oct;13(5):282-90; Neuroscience. 2002;113(2):351-61. |
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