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| 25mg |
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Purity: ≥98%
Udenafil (formerly known as DA8159) is a novel and potent PDE5 inhibitor used in urology to treat erectile dysfunction. It is available for use in Korea, Russia, and Philippines but not in the United States.
| ln Vitro |
Udenafil is a PDE5 inhibitor taken by mouth. In contrast to plasma, udenafil is more widely distributed in the prostate and dramatically raises levels of cAMP and cGMP [1].
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|---|---|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Hepatic. Metabolized by CYP3A4 and CYP3A5. |
| References |
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| Additional Infomation |
Udenafil is a sulfonamide.
Udenafil is a new phosphodiesterase type 5 (PDE5) inhibitor used to treat erectile dysfunction (ED). It has been approved in South Korea and will be marketed under the brand name Zydena. It is not yet approved for use in the U.S., E.U., or Canada. Udenafil is a benzenesulfonamide derivative with vasodilatory activity. Udenafil selectively inhibits phosphodiesterase type 5 (PDE5), thus inhibiting the degradation of cyclic guanosine monophosphate (cGMP) found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis; inhibition of cGMP degradation results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection. This agent does not significantly inhibit the PDE11 isozyme; PDE11 inhibition may be associated with significant myalgia. Drug Indication Investigated for use/treatment in erectile dysfunction and hypertension. Mechanism of Action Udenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by udenafil enhances erectile function by increasing the amount of cGMP. Pharmacodynamics Udenafil is a potent selective phosphodiesterase type 5 (PDE5) inhibitor. |
| Molecular Formula |
C25H36N6O4S
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|---|---|
| Molecular Weight |
516.66
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| Exact Mass |
516.251
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| CAS # |
268203-93-6
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| Related CAS # |
Udenafil-d7;1175992-76-3
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| PubChem CID |
135413547
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| Appearance |
White to off-white solid powder
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| Density |
1.35g/cm3
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| Boiling Point |
697ºC at 760 mmHg(计算值)
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| Melting Point |
157-159°C
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| Flash Point |
375.3ºC(计算值)
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| Vapour Pressure |
2.83E-19mmHg at 25°C(计算值)
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| Index of Refraction |
1.648
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| LogP |
5.606
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
36
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| Complexity |
894
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IYFNEFQTYQPVOC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H36N6O4S/c1-5-8-20-22-23(31(4)29-20)25(32)28-24(27-22)19-16-18(10-11-21(19)35-15-6-2)36(33,34)26-13-12-17-9-7-14-30(17)3/h10-11,16-17,26H,5-9,12-15H2,1-4H3,(H,27,28,32)
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| Chemical Name |
3-(1-methyl-7-oxo-3-propyl-4,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfonamide
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| Synonyms |
DA-8159, DA 8159, DA8159, Udenafil, trade name: Zydena
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 33 mg/mL (~63.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9355 mL | 9.6775 mL | 19.3551 mL | |
| 5 mM | 0.3871 mL | 1.9355 mL | 3.8710 mL | |
| 10 mM | 0.1936 mL | 0.9678 mL | 1.9355 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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