Udenafil
Based on 1 Customer Validation
Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.28%
- CAS. Nr.: 268203-93-6
- Formel: C25H36N6O4S
- Molecular Weight:516.66
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biologische Aktivität
|
PDE5 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
128.2 μM
Compound: Udenafil
|
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| A549 | IC50 |
15.2 μM
Compound: Udenafil
|
Potentiation of cisplatin-induced cytotoxicity against human A549 cells assessed as cisplatin IC50 at 1:5 ratio of cisplatin to compound measured after 48 hrs by MTT assay
Potentiation of cisplatin-induced cytotoxicity against human A549 cells assessed as cisplatin IC50 at 1:5 ratio of cisplatin to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| A549 | IC50 |
150.1 μM
Compound: Udenafil
|
Antiproliferative activity against human A549 cells measured after 24 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 24 hrs by MTT assay
|
[PMID: 39149110] |
| A549 | IC50 |
28.3 μM
Compound: Udenafil
|
Potentiation of raloxifene-induced cytotoxicity against human A549 cells assessed as raloxifene IC50 at 1:3 ratio of raloxifene to compound measured after 48 hrs by MTT assay
Potentiation of raloxifene-induced cytotoxicity against human A549 cells assessed as raloxifene IC50 at 1:3 ratio of raloxifene to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| A549 | IC50 |
82.84 μM
Compound: Udenafil
|
Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
18.8 μM
Compound: Udenafil
|
Potentiation of raloxifene-induced cytotoxicity against human NCI-H1299 cells assessed as raloxifene IC50 at 1:2 ratio of raloxifene to compound measured after 48 hrs by MTT assay
Potentiation of raloxifene-induced cytotoxicity against human NCI-H1299 cells assessed as raloxifene IC50 at 1:2 ratio of raloxifene to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
70.45 μM
Compound: Udenafil
|
Antiproliferative activity against human NCI-H1299 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells measured after 72 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
76.14 μM
Compound: Udenafil
|
Antiproliferative activity against human NCI-H1299 cells measured after 24 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells measured after 24 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
8.2 μM
Compound: Udenafil
|
Potentiation of cisplatin-induced cytotoxicity against human NCI-H1299 cells assessed as cisplatin IC50 at 1:4 ratio of cisplatin to compound measured after 48 hrs by MTT assay
Potentiation of cisplatin-induced cytotoxicity against human NCI-H1299 cells assessed as cisplatin IC50 at 1:4 ratio of cisplatin to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
86.28 μM
Compound: Udenafil
|
Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
177.1 μM
Compound: Udenafil
|
Antiproliferative activity against human NCI-H661 cells measured after 24 hrs by MTT assay
Antiproliferative activity against human NCI-H661 cells measured after 24 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
19.8 μM
Compound: Udenafil
|
Potentiation of raloxifene-induced cytotoxicity against human NCI-H661 cells assessed as raloxifene IC50 at 1:2 ratio of raloxifene to compound measured after 48 hrs by MTT assay
Potentiation of raloxifene-induced cytotoxicity against human NCI-H661 cells assessed as raloxifene IC50 at 1:2 ratio of raloxifene to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
80.35 μM
Compound: Udenafil
|
Antiproliferative activity against human NCI-H661 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human NCI-H661 cells measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
9.6 μM
Compound: Udenafil
|
Potentiation of cisplatin-induced cytotoxicity against human NCI-H661 cells assessed as cisplatin IC50 at 1:4 ratio of cisplatin to compound measured after 48 hrs by MTT assay
Potentiation of cisplatin-induced cytotoxicity against human NCI-H661 cells assessed as cisplatin IC50 at 1:4 ratio of cisplatin to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
98.8 μM
Compound: Udenafil
|
Antiproliferative activity against human NCI-H661 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H661 cells measured after 72 hrs by MTT assay
|
[PMID: 39149110] |
Udenafil is an oral PDE5 inhibitor. Udenafil significantly increases cAMP and cGMP levels and are more highly distributed in the prostate than plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 268203-93-6
-
Appearance Solid
-
Molecular Weight 516.66
-
Formel C25H36N6O4S
-
Color White to off-white
-
SMILES
O=S(C1=CC=C(OCCC)C(C2=NC3=C(N(C)N=C3CCC)C(N2)=O)=C1)(NCCC4N(C)CCC4)=O
-
Synonyms
DA8159
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : ≥ 33 mg/mL (63.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Paick, J.S., et al., The efficacy and safety of udenafil, a new selective phosphodiesterase type 5 inhibitor, in patients with erectile dysfunction. J Sex Med, 2008. 5(4): p. 946-53. [Content Brief]
[2]. Zhao, C., et al., Activity of phosphodiesterase type 5 inhibitors in patients with lower urinary tract symptoms due to benign prostatic hyperplasia. BJU Int, 2011. 107(12): p. 1943-7. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9355 mL | 9.6775 mL | 19.3551 mL | 48.3877 mL |
| 5 mM | 0.3871 mL | 1.9355 mL | 3.8710 mL | 9.6775 mL | |
| 10 mM | 0.1936 mL | 0.9678 mL | 1.9355 mL | 4.8388 mL | |
| 15 mM | 0.1290 mL | 0.6452 mL | 1.2903 mL | 3.2258 mL | |
| 20 mM | 0.0968 mL | 0.4839 mL | 0.9678 mL | 2.4194 mL | |
| 25 mM | 0.0774 mL | 0.3871 mL | 0.7742 mL | 1.9355 mL | |
| 30 mM | 0.0645 mL | 0.3226 mL | 0.6452 mL | 1.6129 mL | |
| 40 mM | 0.0484 mL | 0.2419 mL | 0.4839 mL | 1.2097 mL | |
| 50 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL | |
| 60 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8065 mL |