Vardenafil hydrochloride
- Product Name
- 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
- Formula Weight
- 525.07
- MOL File
- 224785-91-5.mol
Vardenafil hydrochloride Property
- 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
- InChI
- InChI=1S/C23H32N6O4S.ClH/c1-5-8-20-24-16(4)21-23(30)25-22(26-29(20)21)18-15-17(9-10-19(18)33-7-3)34(31,32)28-13-11-27(6-2)12-14-28;/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,30);1H
- 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
- HS Code
- 2933299090
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H311Toxic in contact with skin
H331Toxic if inhaled
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P310Immediately call a POISON CENTER or doctor/physician.
P330Rinse mouth.
P361Remove/Take off immediately all contaminated clothing.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- F755
- Product name
- Vardenafil hydrochloride
- Packaging
- 5mg
- Price
- $29
- Updated
- 2021/12/16
- Product number
- FV28670
- Product name
- Vardenafil hydrochloride
- Packaging
- 50mg
- Price
- $50
- Updated
- 2021/12/16
- Product number
- CS-2765
- Product name
- Vardenafil hydrochloride
- Purity
- 99.51%
- Packaging
- 100mg
- Price
- $84
- Updated
- 2021/12/16
- Product number
- FV28670
- Product name
- Vardenafil hydrochloride
- Packaging
- 250mg
- Price
- $125
- Updated
- 2021/12/16
- Product number
- CS-2765
- Product name
- Vardenafil hydrochloride
- Purity
- 99.51%
- Packaging
- 200mg
- Price
- $151
- Updated
- 2021/12/16
Vardenafil hydrochloride Chemical Properties,Usage,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.
Synthesis
The synthesis started with 2- hydroxybenzonitrile. 2-Hydroxybenzonitrile (181) was alkylated with ethyl bromide to give 2-ethoxybenzonitrile in 97% yield as a liquid which was subsequently treated with AlMeClNH2, prepared from AlMe3 and NH4Cl, to give corresponding 2-ethoxybenzamidine (182) in 76% yield as a solid. Compound 182 was treated with hydrazine hydrate in ethanol to give hydrazide 183, which was used in the next step without isolation. Dakin-West reaction of 2- butyrylaminopropionic acid (184) with ethyl oxalyl chloride (185) in the presence of DMAP in refluxing pyridine/THF to give corresponding |á-oxoamino-acid ester 186 which was also used for next step without isolation. Hydrazide 183 was condensed with ester 186 in refluxing ethanol to give triazinone 187 intermediate which was then cyclized to the final core structure, imidazo[5,1-f]triazin-4-one, using POCl3 to give 188 in 28% yield from 183. Compound 188 was sulfonylated with chlorosulfonic acid to give sulfonyl chloride 189 in 91% yield. Finally, 189 was condensed with N-ethylpiperazine (190) in dichloromethane to give vardenafil (XXIII) in 66% yield.
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.
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.
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
Vardenafil hydrochloride Suppliers
- Tel
- 13345898948
- 1301260554@qq.com
- Country
- China
- ProdList
- 114
- Advantage
- 58
- Tel
- 027-87058617 15872383390
- Fax
- 027-87058617
- hbdibo@163.com
- Country
- China
- ProdList
- 885
- Advantage
- 58
- Tel
- 0515-88981987 13918567443
- Fax
- 0515-88981987
- richard.li_jzchem@263.net
- Country
- China
- ProdList
- 258
- Advantage
- 58
- Tel
- 0531-88072380 0531-88116830 13791093792
- sales@bestcomm.cn
- Country
- China
- ProdList
- 45
- Advantage
- 58
- Tel
- 131-7317-1119 13173171119
- 918582503@qq.com
- Country
- China
- ProdList
- 25
- Advantage
- 58
- Tel
- 171-5642-2032 19587414261
- 3795342424@qq.com
- Country
- China
- ProdList
- 23
- Advantage
- 58
- Tel
- 15926415536 15926415536
- hbcyssw@163.com
- Country
- China
- ProdList
- 33
- Advantage
- 58
- Tel
- 0375-15696900 15696900147
- 3958759419@qq.com
- Country
- China
- ProdList
- 24
- Advantage
- 58
- Tel
- 18062078401
- 290553188@qq.com
- Country
- China
- ProdList
- 139
- Advantage
- 58
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15839
- Advantage
- 69
- Tel
- 010-89508211 18501085097
- Fax
- 010-89508210
- sales.bj@hwrkchemical.com
- Country
- China
- ProdList
- 8418
- Advantage
- 55
- Tel
- 86-29-81325371
- Fax
- +86-29-81325373
- info@everchem.cn
- Country
- China
- ProdList
- 84
- Advantage
- 62
- Tel
- +86-28-61777709
- Fax
- +86-28-61777709
- yygk@yygk.com
- Country
- China
- ProdList
- 69
- Advantage
- 58
- Tel
- 0755-4000505016 13380397412
- Fax
- 0755 28094224
- 3001272453@qq.com
- Country
- China
- ProdList
- 5047
- Advantage
- 50
- Tel
- +86 (21) 5811-6473 5811-6475
- Fax
- +86 (21) 6129-4103
- sales@koutingchina.com
- Country
- China
- ProdList
- 496
- Advantage
- 60
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 027-87666700
- Fax
- 027-87666700 skype-lydia0189
- xuri@hbdatongchem.com
- Country
- China
- ProdList
- 147
- Advantage
- 55
- Tel
- 025-57798810
- Fax
- 025-57019371
- sales@sunlidabio.com
- Country
- China
- ProdList
- 3239
- Advantage
- 55
- Tel
- 021-021-33632979 15002134094
- Fax
- 021-33632979
- marketing@targetmol.com
- Country
- China
- ProdList
- 7783
- Advantage
- 58
- Tel
- 400-8706899
- Fax
- 400-8706899
- hysj_bj.com
- Country
- China
- ProdList
- 3583
- Advantage
- 55
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 400-1166-196 13458535857
- Fax
- QQ：800101999
- cdhxsj@163.com
- Country
- China
- ProdList
- 13350
- Advantage
- 58
- Tel
- 027-87465837 19945049750
- Fax
- 027-8777-2287
- sales@finetechnology-ind.com
- Country
- China
- ProdList
- 9648
- Advantage
- 58
- Tel
- 15221275939 15221275939
- Fax
- 021-50706099
- shenlinxing@macklin.cn
- Country
- China
- ProdList
- 16166
- Advantage
- 55
- Tel
- +86-21-5821 5861
- Fax
- +86-21-5106 2861
- sales@letopharm.com
- Country
- China
- ProdList
- 2384
- Advantage
- 58
- Tel
- Fax
- -
- xg01_gj@163.com
- Country
- China
- ProdList
- 9484
- Advantage
- 50
- Tel
- 18068075658
- Fax
- -
- sales@chempioneer.com
- Country
- China
- ProdList
- 1811
- Advantage
- 58
- Tel
- +86 (531) 8099-2215
- Fax
- +86 (531) 8099-2215
- putubio@outlook.com
- Country
- China
- ProdList
- 1261
- Advantage
- 55
- Tel
- 0571-87157530-8007 13868066926
- Fax
- 0571-87156470
- sales@dingyanchem.com
- Country
- China
- ProdList
- 2190
- Advantage
- 58
- Tel
- 021-50908862，442785678，326799392 18721037013
- Fax
- 021-50908862
- siyansales@126.com
- Country
- China
- ProdList
- 9627
- Advantage
- 58
- Tel
- 18936048580
- chemxilang@163.com
- Country
- China
- ProdList
- 4007
- Advantage
- 58
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 025-83453382-8005
- Fax
- 025-83453382
- sale@parabiochem.com
- Country
- China
- ProdList
- 9595
- Advantage
- 55
- Tel
- sales@njromanme.com
- Country
- China
- ProdList
- 4529
- Advantage
- 58
- Tel
- 010-50973186 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 18338
- Advantage
- 68
- Tel
- 18126413629 0755-23311925 2355327053
- Fax
- 0755-23311925
- abel@ycgmp.com
- Country
- China
- ProdList
- 5113
- Advantage
- 58
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- 0551-65171243 13856024262
- kuer@kuerhuaxue.com
- Country
- China
- ProdList
- 2997
- Advantage
- 55
- Tel
- 15172337137 15172337137
- Fax
- 027-50779735
- 940329747@qq.com
- Country
- China
- ProdList
- 634
- Advantage
- 55
- Tel
- 17792809151
- Fax
- 18872220797
- 2355916837@ycphar.com
- Country
- China
- ProdList
- 6133
- Advantage
- 55
- Tel
- 18800375331
- Fax
- 021-50908862
- kangmansales@163.com
- Country
- China
- ProdList
- 7570
- Advantage
- 55
- Tel
- 13127280945
- 285424065@qq.com
- Country
- China
- ProdList
- 9976
- Advantage
- 55
- Tel
- +86-21-5877 1921
- Fax
- +86-21-5877 1925
- info@chemofchina.com
- Country
- China
- ProdList
- 9653
- Advantage
- 55
- Tel
- 15623071665
- Fax
- 027-59257948
- sales@zvsicom.com
- Country
- China
- ProdList
- 299
- Advantage
- 58
- Tel
- 0512-56316828
- Fax
- 0512-56316826
- info@amateksci.com
- Country
- China
- ProdList
- 28806
- Advantage
- 58
- Tel
- 18578209868 2355327026
- Fax
- 18578209868 QQ：2355327026
- steroidbest@hotmail.com
- Country
- China
- ProdList
- 6501
- Advantage
- 58
- Tel
- 025-58859352 18068836627
- Fax
- 02557626880
- sales01@aikonchem.com
- Country
- China
- ProdList
- 15084
- Advantage
- 58
- Tel
- 021-58958002 18930822973
- Fax
- 021-58958618
- sales@uhnshanghai.com
- Country
- China
- ProdList
- 1942
- Advantage
- 58
- Tel
- 0371-67991738 13783628208
- Fax
- QQ 412703949
- carl@alchemist-pharm.com
- Country
- China
- ProdList
- 1872
- Advantage
- 58
View Lastest Price from Vardenafil hydrochloride manufacturers
- Product
- Vardenafil hydrochloride 224785-91-5
- Price
- US $10.00/ASSAYS
- Min. Order
- 1ASSAYS
- Purity
- 99%
- Supply Ability
- 1 ton
- Release date
- 2024-03-26
- Product
- Vardenafil hydrochloride
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- HPLC≥98%
- Supply Ability
- 1000kg
- Release date
- 2024-03-21
- Product
- vardenafil 224785-91-5
- Price
- US $20.00/kg
- Min. Order
- 1kg
- Purity
- 98%
- Supply Ability
- 2000kg
- Release date
- 2024-05-15