Vardenafil hydrochloride trihydrate

SKU: orb1303165

Description

Vardenafil hydrochloride trihydrate (BAY38-9456) is a selective PDE5 inhibitor with an IC50 of 0.7 nM, showing high selectivity over PDE1 (IC50=180 nM). It is widely used in biochemical research to study erectile dysfunction mechanisms and for in vitro phosphodiesterase activity assays.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	330808-88-3
MW	579.11
Purity	99.89% (May vary between batches)
Formula	C₂₃H₃₂N₆O₄S·HCl·3H₂O
SMILES	O.O.O.Cl.CCCc1nc(C)c2n1nc([nH]c2=O)-c1cc(ccc1OCC)S(=O)(=O)N1CCN(CC)CC1
Target	Endogenous Metabolite,PDE
Solubility	Ethanol:16 mg/mL (27.63 mM);H2O:10 mg/mL (17.27 mM);DMSO:93 mg/mL (160.59 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (5.7 mM)

Bioactivity

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Target IC50	PDE6:11 nM\|PDE3:>1000 nM\|PDE4:>1000 nM\|PDE5:0.7 nM\|PDE1:180 nM
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 the 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.
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.

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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impotence, muscle, Inhibitor, inhibit, PDE1, hepatitis, Endogenous Metabolite, erectile dysfunction, erectile, diabetes, dysfunction, cGMP, BAY38-9456, smooth, stimulation, selective, PDE5, pharmacokinetics, Phosphodiesterase (PDE), Vardenafil, Vardenafil HCl, Vardenafil HCl Trihydrate, Vardenafil hydrochloride, Vardenafil Hydrochloride, Vardenafil hydrochloride Trihydrate, Vardenafil hydrochloride trihydrate, Zucker diabetic fatty (ZDF) rats

Quality Guarantee

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Compound Identifiers

PubChem CID

135413545 ↗

Key Properties

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No computed properties available.

Protocol Information

Find More Protocols

CAS Number:	224785-90-4
MW:	579.1
Formula:	C₂₃H₃₂N₆O₄S.HCl.3(H₂O)

Vardenafil hydrochloride trihydrate

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Vardenafil [orb1972039]

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