Avanafil (Synonyms: TA-1790) |
| Catalog No.GC16856 |
A potent and selective PDE5 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 330784-47-9
Sample solution is provided at 25 µL, 10mM.
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Avanafil is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) with IC50 value of 5.2nM [1].
PDE5 is abundantly expressed in penile corpus cavernosum and regulates penile blood flow by regulating the cGMP concentration. PDE5 inhibitors are similar in structure to cGMP and competitively bind to PDE5, resulting in the inhibition of cGMP hydrolysis. Avanafil is a high selective inhibitor of PDE5 with Ki value of 4.3nM and is developed for the treatment of erectile dysfunction. It shows high selectivity against other PDE enzymes of the PDE family. In the intravenous study, the administration of avanafil at 300μg/kg can potentiate penile tumescence. The calculated ED200% of avanafil on tumescence is 37.5μg/kg and the plasma concentration is 59.6ng/ml. Additionally, avanafil potentiates penile tumescence at a dose range of 100 to 1,000μg/kg intraduodenally. And the ED200% is 151.7μg/kg [1, 2].
References:
[1] Kotera J, Mochida H, Inoue H, Noto T, Fujishige K, Sasaki T, Kobayashi T, Kojima K, Yee S, Yamada Y, Kikkawa K, Omori K. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188(2):668-74.
[2] Cui YS, Li N, Zong HT, Yan HL, Zhang Y. Avanafil for male erectile dysfunction: a systematic review and meta-analysis. Asian J Androl. 2014 May-Jun;16(3):472-7.
| Cas No. | 330784-47-9 | SDF | |
| Synonyms | TA-1790 | ||
| Chemical Name | (S)-4-((3-chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide | ||
| Canonical SMILES | O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4 | ||
| Formula | C23H26ClN7O3 | M.Wt | 483.95 |
| Solubility | ≥ 17.6 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0663 mL | 10.3316 mL | 20.6633 mL |
| 5 mM | 0.4133 mL | 2.0663 mL | 4.1327 mL |
| 10 mM | 0.2066 mL | 1.0332 mL | 2.0663 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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