| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Avanafil (also known as TA 1790; TA1790; TA-1790; trade name: Stendra; Spedra) is a highly potent and selective PDE5 inhibitor with potential vasodilating effects. It inhibits PDE5 with an IC50 of 5.2 nM, and shows >121-fold selectivity for PDE5 over other isoforms of PDE. As of 2012, Avanafil was approved by the US FDA for the treatment of erectile dysfunction.
| ln Vitro |
In corpus cavernosum strips from the diabetic group, avanafil (TA-1790) (0.01-1000 µM) increases the relaxation responses induced by electrical field stimulation (1-20 Hz) by 45%[2].
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| ln Vivo |
Avanafil (TA-1790) (10 mg/kg; po; daily, for 30 d; male rat) dramatically reduces oxidative stress, bone atrophy, and BMD loss caused by dexamethasone while also increasing angiogenesis in bone tissue through the activation of the NO, cGMP, and PKG (NO/cGMP/PKG) signaling pathway[1]. T2DM rats' erectile responses are improved by avanafil (TA-1790) (10 µM; ICI; once, for 10 weeks)[2].
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| Animal Protocol |
Animal/Disease Models: Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
Doses: 10 mg/kg Route of Administration: Oral administration; daily, for 30 days Experimental Results: diminished 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/Disease Models: Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1] Doses: 10 mg/kg Route of Administration: Oral administration; daily, for 30 days Experimental Results: Increased right femur trabecular bone thickness and epiphyseal bone width. Animal/Disease Models: Male T2DM Sprague Dawley rats[2] Doses: 10 µM Route of Administration: Intracavernous injection; once, for 10 weeks Experimental Results: Increased in ICP/MAP in response to nerve stimulation and increased total ICP values. |
| References |
[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.
[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. [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. |
| Molecular Formula |
C23H26CLN7O3
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|---|---|
| Molecular Weight |
483.95
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| CAS # |
330784-47-9
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| Related CAS # |
Avanafil dibenzenesulfonate;330784-48-0;(R)-Avanafil;1638497-26-3;Avanafil-13C,d3
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| SMILES |
O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4
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| InChi Key |
WEAJZXNPAWBCOA-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C23H26ClN7O3/c1-34-19-6-5-15(10-18(19)24)11-27-21-17(22(33)28-13-20-25-7-3-8-26-20)12-29-23(30-21)31-9-2-4-16(31)14-32/h3,5-8,10,12,16,32H,2,4,9,11,13-14H2,1H3,(H,28,33)(H,27,29,30)/t16-/m0/s1
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| Chemical Name |
(S)-4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2pyrimidinylmethyl)-5-pyrimidinecarboxamide
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| Synonyms |
TA 1790; TA1790; Avanafil; TA-1790; trade name: Stendra; Spedra
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.17 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 (5.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04374994 | Completed | Drug: Avanafil 50 MG Drug: Placebo oral tablet |
Erectile Dysfunction | University of Alexandria | September 1, 2018 | Phase 4 |
| NCT01054430 | Completed | Drug: avanafil | Erectile Dysfunction | VIVUS LLC | January 2010 | Phase 1 |
| NCT01095601 | Completed | Drug: Avanafil | Healthy | VIVUS LLC | April 2010 | Phase 1 |
| NCT01054261 | Completed | Drug: avanafil | Renal | VIVUS LLC | January 2010 | Phase 1 |
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