| CAS NO: | 224785-90-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| Molecular Weight (MW) | 488.6 |
|---|---|
| Formula | C23H32N6O4S |
| CAS No. | 224785-90-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mM |
| Water: N/A | |
| Ethanol: N/A | |
| Solubility (In vivo) | Chemical Name: 2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propyl-3,5,6,7-tetrahydro-4H-5l4-imidazo[1,5-a][1,3,5]triazin-4-one InChi Key: UWRWYSQUBZFWPU-UHFFFAOYSA-N InChi Code: InChI=1S/C23H35N6O4S/c1-5-10-27-16-21-24-22(25-23(30)29(21,4)17-27)19-15-18(8-9-20(19)33-7-3)34(31,32)28-13-11-26(6-2)12-14-28/h8-9,15-16H,5-7,10-14,17H2,1-4H3,(H,24,25,30) SMILES Code: O=C(NC(C1=CC(S(=O)(N2CCN(CC)CC2)=O)=CC=C1OCC)=N3)[N]4(C)C3=CN(CCC)C4 |
| Synonyms | BAY38-9456; BAY 38-9456; BAY-38-9456; BAY38-9456;trade names: 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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