Amino Tadalafil |
Catalog No.GC10859
One-Click Copy Product Info
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analog of tadalafil, a potent inhibitor of phosphodiesterase 5
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 385769-84-6
Sample solution is provided at 25 µL, 10mM.
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Amino tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5).
PDE5, an enzyme found primarily in the smooth muscle of the corpus cavernosum, selectively cleaves and degrades cGMP to 5′-GMP. PDE5 inhibitors are similar in structure to cGMP and they competitively bind to PDE5 and inhibit cGMP hydrolysis, thus enhancing the effects of NO, resulting in prolonging an erection.
In vitro: Amino-tadalafil is a structural analogue of tadalafil, the active pharmaceutical ingredient in Cialis, a prescription drug approved in the US for treatment of erectile dysfunction (ED). Similarly, there have also been reports of herbal or dietary supplements being adulterated with designer ED analogues such as amino-tadalafil [1].
In vivo: In rats treated with both melatonin and tadalafil, the recoveries were more pronounced than in rats given either melatonin or tadalafil alone. The ICP/mean arterial pressure value in vehicle-treated rats was significantly higher than in the control group, while in the tadalafil- and tadalafil + melatonin-treated groups have returned this value had returned to control levels. In addition, as an individual treatment, and especially when combined with tadalafil, melatonin prevented spinal cord injury (SCI)-induced oxidative damage to cavernosal tissues and restored ED, most likely due to its anti-oxidant effects [2].
Clinical trial: Up to now, amino tadalafil is still in the preclinical development stage.
References:
[1] Hadwiger ME, Trehy ML, Ye W, Moore T, Allgire J, Westenberger B. Identification of amino-tadalafil and rimonabant in electronic cigarette products using high pressure liquid chromatography with diode array and tandem mass spectrometric detection. J Chromatogr A. 2010 Nov 26;1217(48):7547-55.
[2] Tavuk u HH, Sener TE, Tinay I, Akbal C, Er ahin M, Cevik O, Cadirci S, Reiter RJ, Sener G. Melatonin and tadalafil treatment improves erectile dysfunction after spinal cord injury in rats. Clin Exp Pharmacol Physiol. 2014 Apr;41(4):309-16.
| Cas No. | 385769-84-6 | SDF | |
| Chemical Name | (6R,12aR)-2-amino-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione | ||
| Canonical SMILES | O=C1N(N)CC(N2[C@H](C3=CC=C(OCO4)C4=C3)C5=C(C6=CC=CC=C6N5)C[C@@]21[H])=O | ||
| Formula | C21H18N4O4 | M.Wt | 390.4 |
| Solubility | ≤15mg/ml in DMSO;15mg/ml in dimethyl formamide | 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 | 2.5615 mL | 12.8074 mL | 25.6148 mL |
| 5 mM | 512.3 μL | 2.5615 mL | 5.123 mL |
| 10 mM | 256.1 μL | 1.2807 mL | 2.5615 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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)