Vardenafil HCl Trihydrate

Catalog No.S2515 Batch:S251501

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Technical Data

Formula

C23H32N6O4S.HCl.3H2O

Molecular Weight 579.11 CAS No. 330808-88-3
Solubility (25°C)* In vitro DMSO 116 mg/mL (200.3 mM)
Water 116 mg/mL (200.3 mM)
Ethanol 20 mg/mL (34.53 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
Targets
PDE5 [1]
(Cell-free assay)
0.7 nM
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. [1] Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. [2] Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle. [3]
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. [2] 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. [4] 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. [5]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Cancer Lett, 2016, 378(1):38-50.]

Data from [Data independently produced by , , Oncotarget, 2017, 8(5):8574-8589]

Selleck's Vardenafil HCl Trihydrate has been cited by 11 publications

Impaired Redox and Protein Homeostasis as Risk Factors and Therapeutic Targets in Toxin-Induced Biliary Atresia [ Gastroenterology, 2020, 159(3):1068-1084.e2] PubMed: 32505743
Skeletal restoration by phosphodiesterase 5 inhibitors in osteopenic mice: Evidence of osteoanabolic and osteoangiogenic effects of the drugs. [ Bone, 2020, 10.1016/j.bone.2020.115305] PubMed: 32126313
Evaluation of the combination of endothelin receptor antagonists (ERA) and phosphodiesterase-5 inhibitors for the treatment of pulmonary arterial hypertension (PAH) in pathologic human pulmonary arteries in an ex-vivo organ bath model [ Pulm Pharmacol Ther, 2020, 66:101985] PubMed: 33359621
Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression. [ Cancers (Basel), 2019, 11(11)] PubMed: 31698786
Effect of RAD51C expression on the chemosensitivity of Eμ-Myc p19Arf-/- cells and its clinical significance in breast cancer [ Oncol Lett, 2018, 15(5):6107-6114] PubMed: 29731842
FOXM1 evokes 5-fluorouracil resistance in colorectal cancer depending on ABCC10. [Xie T, et al. Oncotarget, 2017, 8(5):8574-8589] PubMed: 28051999
Phosphodiesterase Inhibitors Sildenafil and Vardenafil Reduce Zebrafish Rod Photoreceptor Outer Segment Shedding. [ Invest Ophthalmol Vis Sci, 2017, 58(13):5604-5615] PubMed: 29094165
Phosphodiesterase 5/protein kinase G signal governs stemness of prostate cancer stem cells through Hippo pathway. [Liu N, et al. Cancer Lett, 2016, 378(1):38-50] PubMed: 27179930
Repurposing FDA-approved drugs for anti-aging therapies. [ Biogerontology, 2016, 17(5-6):907-920] PubMed: 27484416
Inhibition of phosphodiesterase 5 reduces bone mass by suppression of canonical Wnt signaling. [Gong Y, et al. Cell Death Dis, 2014, 5:e1544] PubMed: 25429621

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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