GRADE & PURITY 10mM in DMSO

Synonyms

BAY38-9456 | 2-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl)-5-methyl-7-propylimidazo[1,5-f][1,2,4]triazin-4(3H)-one hydrochloride trihydrate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
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. 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.

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. 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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

BAY38-9456 | 2-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl)-5-methyl-7-propylimidazo[1, 5-f][1, 2, 4]triazin-4(3H)-one hydrochloride trihydrate

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Nombres e identificadores

• Isómeros SMILES: CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C.O.O.O.Cl
• CAS alternativo: 224785-90-4，224785-91-5
• PubChem CID: 135413545
• Peso molecular: 579.11

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 74 mg/mL (200.34 mM); Water: Insoluble; Ethanol: Insoluble

Referencias

1. Ma Yufeng, Zhang Fengsen, Zhong Yijing, Huang Yongchun, Yixizhuoma , Jia Qiangqiang, Zhang Shoude.  (2023)  A label-free LC/MS-based enzymatic activity assay for the detection of PDE5A inhibitors.  Frontiers in Chemistry,      [PMID:36860644] [10.3389/fchem.2023.1097027]