2. Metabolic Enzyme/Protease Others
  3. Phosphodiesterase (PDE) Endogenous Metabolite Isotope-Labeled Compounds
  4. Vardenafil-d5 hydrochloride

Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].

For research use only. We do not sell to patients.

Vardenafil-d<sub>5</sub> hydrochloride

Vardenafil-d5 hydrochloride Chemical Structure

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Vardenafil-d5 hydrochloride Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4[1]. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels[2]. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Vardenafil hydrochloride specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM[2].
Vardenafil hydrochloride increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the body's sinuses and blood flow[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Vardenafil-d5 hydrochloride Related Antibodies
In Vivo

Vardenafil hydrochloride (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury[5].
Vardenafil hydrochloride (I.V.; 0.17 mg/kg once daily; 7 days) protects liver against Con A–induced hepatitis, and decreases the expression of NF-[6].
Vardenafil hydrochloride (P.O.; 10 mg/kg once daily; 25 weeks) prevents the reduction of tissue cGMP levels and the increase in 3-NT generation in ZDF hearts[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

530.09

Formula

C23H28D5ClN6O4S
Unlabeled CAS
Appearance

Solid

Color

White to off-white

SMILES

CC1=C2N(NC(C3=CC(S(=O)(N4CCN(CC4)C([2H])(C([2H])([2H])[2H])[2H])=O)=CC=C3OCC)=NC2=O)C(CCC)=N1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (188.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8865 mL 9.4324 mL 18.8647 mL
5 mM 0.3773 mL 1.8865 mL 3.7729 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8865 mL 9.4324 mL 18.8647 mL 47.1618 mL
5 mM 0.3773 mL 1.8865 mL 3.7729 mL 9.4324 mL
10 mM 0.1886 mL 0.9432 mL 1.8865 mL 4.7162 mL
15 mM 0.1258 mL 0.6288 mL 1.2576 mL 3.1441 mL
20 mM 0.0943 mL 0.4716 mL 0.9432 mL 2.3581 mL
25 mM 0.0755 mL 0.3773 mL 0.7546 mL 1.8865 mL
30 mM 0.0629 mL 0.3144 mL 0.6288 mL 1.5721 mL
40 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1790 mL
50 mM 0.0377 mL 0.1886 mL 0.3773 mL 0.9432 mL
60 mM 0.0314 mL 0.1572 mL 0.3144 mL 0.7860 mL
80 mM 0.0236 mL 0.1179 mL 0.2358 mL 0.5895 mL
100 mM 0.0189 mL 0.0943 mL 0.1886 mL 0.4716 mL
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Vardenafil-d5 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vardenafil-d5Phosphodiesterase (PDE)Endogenous MetaboliteIsotope-Labeled CompoundscGMPselectivesmoothmuscleNOstimulationerectiledysfunctionVardenafilimpotencepharmacokineticserectile dysfunctionhepatitisZucker diabetic fatty (ZDF) ratsdiabetesInhibitorinhibitorinhibit

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