Vardenafil hydrochloride
- CAS No.
- 224785-91-5
- Chemical Name:
- Vardenafil hydrochloride
- Synonyms
- VARDENAFIL HCL;Vardenafi;Nuviva;fafinafei;Valdenafil;Levitra, Valdenafil;vardenafil USP/EP/BP;Levitra,Valdenafil.HCl;Varden?l Hydrochloride;Vardenafil 224785-91-5
- CBNumber:
- CB6672278
- Molecular Formula:
- C23H33ClN6O4S
- Molecular Weight:
- 525.07
- MOL File:
- 224785-91-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2025/4/22 8:33:01
| Melting point | 214-216°C |
|---|---|
| storage temp. | Store at -20°C |
| solubility | DMSO: 100 mg/mL (190.45 mM); Water: ≥ 100 mg/mL (190.45 mM) |
| form | Solid |
| color | White to Off-White Cyrstalline |
| InChIKey | XCMULUAPJXCOHI-UHFFFAOYSA-N |
| SMILES | C(C1=NC(C)=C2C(N=C(C3C=C(S(N4CCN(CC)CC4)(=O)=O)C=CC=3OCC)NN12)=O)CC.Cl |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS06 |
|---|---|
| Signal word | Danger |
| Hazard statements | H301-H311-H331 |
| Precautionary statements | P261-P264-P270-P271-P280-P302+P352-P304+P340-P310-P330-P361-P403+P233-P405-P501 |
| HS Code | 2933299090 |
Vardenafil hydrochloride Chemical Properties,Uses,Production
Description
Vardenafil was the second agent to be marketed and had the advantage that its onset time was not reduced by taking the medication on a full stomach . It is 30 times more potent as an inhibitor of PDE5 (mean IC50, 3.9 nM) than sildenafil and 10 times more potent than tadalafil, with a greater selectivity (>1,000 times) for human PDE5 than for human PDE2, PDE3, and PDE4 and moderate selectivity (>80 times) for PDE1. The PDE inhibitory selectivity and both the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5, with an IC50 of 0.7 nM (sildenafil 6.6 nM). The IC50 of vardenafil for PDE1 was 180 nM, for PDE6 11 nM, and for PDE2, PDE3 and PDE4 more than 1,000 nM.
Chemical Properties
White to Off-White Cyrstalline Solid
Uses
vardenafil hydrochloride is a selective phsphodiesterase type 5 (pde5) inhibitor that is used as a urological agent in the treatment of erectile dysfunction.
General Description
Vardenafil, 4-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4.3.0]nona-3,7,9-trien-2-one(Levitra), was the second PDE5 introduced in the U.S. market.The metabolism of vardenafil is primarily by CYP3A4.As such, concomitant use of CYP3A4 inhibitors such as ritonavir,indinavir, ketoconazole, as well as moderate CYP3Ainhibitors such as erythromycin typically results in significantincreases of plasma levels of vardenafil.
in vitro
Vardenafil hydrochloride specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM. 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.
Enzyme inhibitor
Vardenafil also is rapidly absorbed and peaks in concentration (9.05 μg/mL after a 10-mg dose) after 0.9 hours, displaying a half-life of 4 to 5 hours. The absorption rate of both sildenafil and vardenafil are reduced when taken with a high-fat diet. The drug also is metabolized by hepatic CYP3A4, and a potential for drug–drug interaction with inhibitors or enhancers of CYP3A4 exists. Biochemical studies demonstrate a significant increase in selectivity of vardenafil over sildenafil for PDE5 versus PDE6. Whether this translates into a significant improvement in side effects must await studies in a greater population of patients.
in vivo
Vardenafil hydrochloride (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury.
Vardenafil hydrochloride (I.V.; 0.17 mg/kg once daily for 7 days) protects the liver against Con A-induced hepatitis and decreases the expression of NF--.
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.
Vardenafil hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Alembic Pharmaceuticals Limited | +91-2652280880 +91-2652280550 | Gujarat, India | 115 | 58 | Inquiry |
| BDR Pharmaceuticals International Pvt Ltd | +91-2240560560 +91-7718884418 | Maharashtra, India | 206 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6514 | 58 | Inquiry |
| Vulcan Industrial Engineering Company Private Limited | 08068441081Ext 186 | Gujarat, India | 8 | 58 | Inquiry |
| Clinse Labs Private Limited. | +091-40-23778611 | New Delhi, India | 372 | 30 | Inquiry |
| ALEMBIC PHARMACEUTICALS LTD | +91 40 23704923 / 24 / 25 | New Delhi, India | 108 | 58 | Inquiry |
| Hubei Chuyunshun Biotechnology Co., Ltd. | +86-15926415536 +86-15926415536 | China | 160 | 58 | Inquiry |
| Firsky International Trade (Wuhan) Co., Ltd | +8615387054039 | China | 427 | 58 | Inquiry |
| Wuhan Ruichi Technology Co., Ltd | +8613545065237 | China | 153 | 58 | Inquiry |
| Nantong Guangyuan Chemicl Co,Ltd | +undefined17712220823 | China | 615 | 58 | Inquiry |
Related articles
- Vardenafil Hydrochloride: Pharmacodynamics and Methods of Preparation
- Vardenafil hydrochloride effectively treats erectile dysfunction by enhancing cGMP levels, offering higher potency and tolerab....
- Feb 19，2024
- Vardenafil hydrochloride: Pharmacokinetics, Mechanism and Synthesis
- Vardenafil hydrochloride is an oral medication that is typically used to treat erectile dysfunction (ED) in men, which helps e....
- Apr 26，2023
- Medical use and Precautions of Vardenafil hydrochloride
- Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guano....
- Oct 9，2019