| Tadalafil Catalog No.GC17074 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
| Cell experiment [1]: | |
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Cell lines |
human hepatocytes |
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Preparation method |
The solubility of this compound in DMSO is >16.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1 μM |
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Applications |
Tadalafil (1 μM) increased CYP3A protein expression in human hepatocytes. |
| Animal experiment [2,3]: | |
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Animal models |
Rat model with bilateral cavernous neurotomy (BCN)-induced penile damage and hypo-oxygenation, Mice with cavernous nerve resection |
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Dosage form |
2 mg/kg, daily for 3 months |
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Application |
Tadalafil (2 mg/kg) almost completely restored penile oxygenation and abolished neurotomy induced increase and substantially rescued muscle/fiber ratio in penile sectionsin sham-operated rats. Tadalafil decreased the number of apoptotic cells and increased the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Ring B J, Patterson B E, Mitchell M I, et al. Effect of tadalafil on cytochrome P450 3A4–mediated clearance: studies in vitro and in vivo[J]. Clinical Pharmacology & Therapeutics, 2005, 77(1): 63-75. [2]. Morelli A, Vignozzi V, Filippi S, et al. Effect of Chronic Tadalafil Administration on Penile Hypoxia Induced by Cavernous Neurotomy in the Rat[J]. The Journal of Sexual Medicine, 2006, 3: 46. [3]. Lysiak J J, Yang S K, Klausner A P, et al. Tadalafil increases Akt and extracellular signal-regulated kinase 1/2 activation, and prevents apoptotic cell death in the penis following denervation[J]. The Journal of urology, 2008, 179(2): 779-785. | |
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| Cas No. | 171596-29-5 | SDF | |
| Synonyms | Cialis,ICOS 351,Ic351,IC 351,IC-351 | ||
| Chemical Name | (6R,12aR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6H,7H)-dione | ||
| Canonical SMILES | O=C1N(C)CC(N([C@@H]2C(C=C3)=CC4=C3OCO4)[C@]1([H])CC5=C2NC6=CC=CC=C56)=O | ||
| Formula | C22H19N3O4 | M.Wt | 389.4 |
| Solubility | ≥16.6 mg/mL in DMSO, <2.81 mg/mL in EtOH, <2.09 mg/mL in H2O | Storage | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Tadalafil, also known as IC351 or Cialis, is a potent, reversible and competitive small-molecule inhibitor of phosphodiesterase 5 (PDE5), a predomiant PDE in the pulmonary vasculature that hydrolyzes cyclic guanosine monophosphate (cGMP) and is involved in the pathobiology of pulmonary arterial hypertension (PAH). The inhibitory effect of tadalafil is PDE5 specific with the selectivity of 10000 times greater than that of PDE1, PDE4, PDE7, PDE8, PDE9 and PDE10 and of 780 times greater than that of PDE6. Although it is used for the treatment of erectile dysfunction through oral administration, tadalafil also improves the vasoconstrictive-predominate condition of PAH through elevating cGMP levels in pulmonary vessels resulted from PDE5 inhibition.
Reference
[1].Fusae Sawamura, Masami Kato, Kazushisa Fujita, Takahiro Nakazawa and Anthony Bearsworth. Tadalafil, a long-acting inhibitor of PDE5, improves pulmonary hemodynamics and survival rate of monocrotaline-induced pulmonary artery hypertension in rats. J Pharmacol Sci 111, 235-243 (2009)
[2].H Porst. IC351 (tadalafil, Cialis): update on clinical experience. Internation Journal of Impotence Research (2002) 14, Suppl 1, S57-S64
[3].S. Thomas Forgue, Beverley E. Patterson, Alun W. Bedding, Christopher D. Payne, Diane L. Phillips, Rebecca E. Wrishko and Malcolm I. Mitchell. Tadalafil pharmacokinetics in healthy subjects. Br J Clin Pharmacol (2005); 61(3): 280-288