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;Vardenafil 224785-91-5;Vardenafil / Vardenafil
- CBNumber:
- CB6672278
- Molecular Formula:
- C23H33ClN6O4S
- Molecular Weight:
- 525.07
- MOL File:
- 224785-91-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/5/15 13:17:26
| 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.
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.
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 |
| Mylan Laboratories Ltd | +91-4023550543 +91-4030866666 | Telangana, India | 150 | 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 |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Vulcan Industrial Engineering Company Private Limited | 08068441081Ext 186 | Gujarat, India | 8 | 58 | Inquiry |
| Firsky International Trade (Wuhan) Co., Ltd | +8615387054039 | China | 436 | 58 | Inquiry |
| Hebei Mojin Biotechnology Co., Ltd | +8613288715578 | China | 12456 | 58 | Inquiry |
| Wuhan Ruichi Technology Co., Ltd | +8613545065237 | China | 161 | 58 | Inquiry |
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