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Vardenafil HCl Trihydrate

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InvivoChem Cat #: V0781

CAS #: 330808-88-3 Purity ≥98%

Description: Vardenafil HCl Trihydrate, also known as BAY 38-9456, is a novel PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil is used for treating erectile dysfunction. Vardenafil (VAR) is synthetic, highly selective, and potent inhibitor of phosphodiesterase-5 which competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. It is clinically approved for treatment of erectile dysfunction in men, including diabetic and postprostatectomy patients.

References: Int J Impot Res. 2001 Oct;13(5):282-90; Neuroscience. 2002;113(2):351-61.

Related CAS: 224785-90-4 (free base); 330808-88-3 (HCl trihydrate); 224789-15-5 (2HCl)

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Molecular Weight (MW)	579.11
Formula	C23H32N6O4S.HCl.3H2O
CAS No.	330808-88-3 (HCl trihydrate);
Storage	-20℃ for 3 years in powder form
Storage	-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

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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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Purity ≥ 98%
COA
MDSD
NMR

Potency of inhibition of PDE catalytic activity by PDE5 inhibitors. Affinity of PDE5 for binding 3H inhibitors.Mol Pharmacol. 2004 Jul;66(1):144-52.	Effects of nucleotides and inhibitors on binding of 3H inhibitors to PDE5. Mol Pharmacol. 2004 Jul;66(1):144-52. Effect of cGMP on [3H]vardenafil binding at 4° and 30°C. Mol Pharmacol. 2004;66(1):144-52.	Dissociation of 3H inhibitors from PDE5 after infinite dilution. Mol Pharmacol.2004 Jul;66(1):144-52.

Vardenafil HCl Trihydrate

Affinity of PDE5 for binding 3H inhibitors.Mol Pharmacol. 2004 Jul;66(1):144-52.

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