Avanafil
Based on 1 publication(s) in Google Scholar
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.00%
- CAS 番号: 330784-47-9
- 分子式: C23H26ClN7O3
- 分子量:483.95
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Anti-diabetic Compound Library
HY-L040
-
Oxygen Sensing Compound Library
HY-L045
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Endocrinology Compound Library
HY-L047
-
NMPA-Approved Drug Library
HY-L053
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neuroprotective Compound Library
HY-L070
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Angiogenesis-Related Compound Library
HY-L088
-
Targeted Diversity Library
HY-L099
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Human Metabolite Library
HY-L123
-
Heterocyclic Compound Library
HY-L138
-
Off-patent Drug Library
HY-L141
-
Mitochondrial Protection Compound Library
HY-L144
-
Antihypertensive Compound Library
HY-L145
-
Metabolic Enzyme Compound Library
HY-L146
-
Membrane Protein-targeted Compound Library
HY-L149
-
Highly Selective Inhibitors Library
HY-L158
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
RO5 Drug-like Natural Product Library
HY-L200
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Natural Product Diversity Scaffold Library
HY-L245
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
FDA-Approved Drug Library
HY-L022
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
MedChemExpress（MCE）の使用を引用している文献 Avanafil
MoreEndogenous Metabolite アイソフォーム固有の製品をすべて表示
More
生物活性
|
PDE5 5.2 nM (IC50) |
PDE6 630 nM (IC50) |
PDE4 5700 nM (IC50) |
PDE10 6200 nM (IC50) |
PDE7 27000 nM (IC50) |
PDE2 51000 nM (IC50) |
PDE1 53000 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
12.3 μM
Compound: Avanafil
|
Potentiation of cisplatin-induced cytotoxicity against human A549 cells assessed as cisplatin IC50 at 1:7 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 1:7 ratio of cisplatin to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| A549 | IC50 |
127.3 μM
Compound: Avanafil
|
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 |
131.2 μM
Compound: Avanafil
|
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] |
| A549 | IC50 |
170.5 μM
Compound: Avanafil
|
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 |
23.3 μM
Compound: Avanafil
|
Potentiation of raloxifene-induced cytotoxicity against human A549 cells assessed as raloxifene IC50 at 1:4 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 1:4 ratio of raloxifene to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
15 μM
Compound: Avanafil
|
Potentiation of raloxifene-induced cytotoxicity against human NCI-H1299 cells assessed as raloxifene IC50 at 1:5 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 1:5 ratio of raloxifene to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H1299 | IC50 |
161.6 μM
Compound: Avanafil
|
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 |
169.1 μM
Compound: Avanafil
|
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 |
184.4 μM
Compound: Avanafil
|
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-H1299 | IC50 |
7.1 μM
Compound: Avanafil
|
Potentiation of cisplatin-induced cytotoxicity against human NCI-H1299 cells assessed as cisplatin IC50 at 1:9 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 1:9 ratio of cisplatin to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
16.4 μM
Compound: Avanafil
|
Potentiation of raloxifene-induced cytotoxicity against human NCI-H661 cells assessed as raloxifene IC50 at 1:5 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 1:5 ratio of raloxifene to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
| NCI-H661 | IC50 |
186.2 μM
Compound: Avanafil
|
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 |
264 μM
Compound: Avanafil
|
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 |
78.52 μM
Compound: Avanafil
|
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] |
| NCI-H661 | IC50 |
8.2 μM
Compound: Avanafil
|
Potentiation of cisplatin-induced cytotoxicity against human NCI-H661 cells assessed as cisplatin IC50 at 1:9 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 1:9 ratio of cisplatin to compound measured after 48 hrs by MTT assay
|
[PMID: 39149110] |
Avanafil (TA-1790) (0.01-1000 μM) enhances by 45% for electrical field stimulation (1-20 Hz)-induced relaxation responses in corpus cavernosum strips from the diabetic group[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Avanafil (TA-1790) (10 μM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
-
Dosage:10 mg/kg
-
Administration:Oral administration; daily, for 30 days
-
Result:Decreased the level of eNOS, NO, PDE-5, PICP, MDA, CoQ10/CoQ10H and 8-OHdG/108dG. Increased the level of cGMP, PKG, Cortisol and CTCP.
-
Animal Model:Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
-
Dosage:10 mg/kg
-
Administration:Oral administration; daily, for 30 days
-
Result:Increased right femur trabecular bone thickness and epiphyseal bone width.
-
Animal Model:Male T2DM Sprague Dawley rats[2]
-
Dosage:10 µM
-
Administration:Intracavernous injection; once, for 10 weeks
-
Result:Increased in ICP/MAP in response to nerve stimulation and increased total ICP values.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 330784-47-9
-
性状 Solid
-
分子量 483.95
-
分子式 C23H26ClN7O3
-
Color White to off-white
-
SMILES
COC1=C(Cl)C=C(CNC2=C(C(NCC3=NC=CC=N3)=O)C=NC(N4[C@H](CO)CCC4)=N2)C=C1
-
別名
TA1790
-
Structure Classification
-
Initial Source
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
溶剤 & 溶解度
DMSO : 14.29 mg/mL (29.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (5.17 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.17 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション
-
データシート (282 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Huyut Z, et, al. Effects of the Phosphodiesterase-5 (PDE-5) Inhibitors, Avanafil and Zaprinast, on Bone Remodeling and Oxidative Damage in a Rat Model of Glucocorticoid-Induced Osteoporosis. Med Sci Monit Basic Res. 2018 Mar 13;24:47-58. [Content Brief]
[2]. Yilmaz D, et, al. The effect of intracavernosal avanafil, a newer phosphodiesterase-5 inhibitor, on neonatal type 2 diabetic rats with erectile dysfunction. Urology. 2014 Feb;83(2):508.e7-12. [Content Brief]
[3]. Kotera J, et, al. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188(2):668-74. [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 | 2.0663 mL | 10.3316 mL | 20.6633 mL | 51.6582 mL |
| 5 mM | 0.4133 mL | 2.0663 mL | 4.1327 mL | 10.3316 mL | |
| 10 mM | 0.2066 mL | 1.0332 mL | 2.0663 mL | 5.1658 mL | |
| 15 mM | 0.1378 mL | 0.6888 mL | 1.3776 mL | 3.4439 mL | |
| 20 mM | 0.1033 mL | 0.5166 mL | 1.0332 mL | 2.5829 mL | |
| 25 mM | 0.0827 mL | 0.4133 mL | 0.8265 mL | 2.0663 mL |
Avanafil 関連分類
HY-18252 関連分類
Powered by Bioz