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Purity: ≥98%
Description: Tadalafil (formerly known as IC351; IC-351; trade name Cialis) is a potent, orally bioavailable, reversible and competitive small-molecule inhibitor of PDE-5 (phosphodiesterase 5) with the potential to treat erectile dysfunction (ED), benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension. It inhibits PDE5 with an IC50 of 1.8 nM in a cell-free assay, and shows >10000-fold selectivity for PDE5 over other isoforms of PDE such as PDE1/47/8/9/10. Tadalafil is mainly used for the treatment of erectile dysfunction (ED) via oral administration, but also improves the vasoconstrictive-predominate condition of PAH through elevating cGMP levels in pulmonary vessels resulted from PDE5 inhibition, therefore, it is also a medication used to treat benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension.
| ln Vitro |
The assays IC (50), K (D) (isotherm), K (D) (dissociation rate), and K (D) ((1/2) EC (50)) were utilized to ascertain the biochemical potency (affinity) of these compounds for PDE5. The results showed that the following compounds met the criteria: sildenafil (3.7 +/-1.4, 4.8 +/-0.80, 3.7 +/-0.29 and 11.7 +/-0.70 nM), Tadalafil (1.8 +/-0.40, 2.4 +/-0.60, 1.9 +/-0.37 and 2.7 +/-0.25 nM); and vardenafil (0.091 +/-0.031, 0.38 +/-0.07, 0.27 +/-0.01 and 0.42 +/-0.10 nM). As a result, each inhibitor has comparable absolute potency values, with vardenafil having the highest relative potency followed by tadalafil and sildenafil [1]. The semen samples were mixed with 0.5 ml of Tadalafil solutions at varying concentrations (0.2, 0.1, 0.05, and 0.025 μg ml-1, respectively). After two hours of incubation, samples treated with 0.2 μg ml-1 Tadalafil demonstrated a significant increase in sperm motility in both groups [2].
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| ln Vivo |
The Tadalafil-treated group's erectile function (intocavernosal pressure/mean arterial pressure) at 0.3, 0.5, 1, 3, and 5 Hz was higher than the diabetic group's values at comparable frequencies that were near to the control values [3]. Orally administer 20 mg of Tadalafil or 100 mg of Sildenafil. In neither group were there statistically significant variations in the parameters of computer-assisted semen analysis. After taking sildenafil for one hour and tadalafil for two hours, there was no discernible change in the frequency of acrosome preterm response [2].
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| References |
[1]. Blount MA, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency,specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52.
[2]. Yang Y, et al. Effect of acute tadalafil on sperm motility and acrosome reaction: in vitro and in vivo studies. Andrologia. 2013 Apr 14. [Epub ahead of print] [3]. Mostafa ME, et al. Effect of Chronic Low-dose Tadalafil on Penile Cavernous Tissues in Diabetic Rats. Urology. 2013 Jun;81(6):1253-60. |
| Molecular Formula |
C22H19N3O4
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|---|---|
| Molecular Weight |
389.4
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| CAS # |
171596-29-5
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| Related CAS # |
Nortadalafil;171596-36-4;cis-Tadalafil;171596-27-3;ent-Tadalafil;629652-72-8;cis-ent-Tadalafil;171596-28-4;Tadalafil-d3;960226-55-5
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| SMILES |
O=C([C@@]1([H])CC2=C([C@@H](C3=CC(OCO4)=C4C=C3)N15)NC6=C2C=CC=C6)N(C)CC5=O
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| InChi Key |
WOXKDUGGOYFFRN-IIBYNOLFSA-N
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| InChi Code |
InChI=1S/C22H19N3O4/c1-24-10-19(26)25-16(22(24)27)9-14-13-4-2-3-5-15(13)23-20(14)21(25)12-6-7-17-18(8-12)29-11-28-17/h2-8,16,21,23H,9-11H2,1H3/t16-,21-/m1/s1
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| Chemical Name |
(6R,12aR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
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| Synonyms |
C-351; IC 351; Tadalafil; IC351; Trade names: Adcirca, Cialis
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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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5681 mL | 12.8403 mL | 25.6805 mL | |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1361 mL | |
| 10 mM | 0.2568 mL | 1.2840 mL | 2.5681 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.
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