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    Tadalafil
    Tadalafil

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0780
    CAS #: 171596-29-5 Purity ≥98%

    Description: Tadalafil (also known as IC351 or Cialis-trade name) is a potent, orally bioavailable, reversible and competitive small-molecule inhibitor of PDE-5 with IC50 of 1.8 nM in a cell-free assay. 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 (ED) through oral administration, tadalafil also improves the vasoconstrictive-predominate condition of PAH through elevating cGMP levels in pulmonary vessels resulted from PDE5 inhibition. It is also a medication used to treat benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension.

    ReferencesMol Pharmacol. 2004;66(1):144-52; Clin Pharmacol Ther. 2005;77(1):63-75; J Sex Med. 2006;3(3):419-31.

    Related CAS: 385769-84-6 (Aminotadalafil); 171596-27-3 [Tadalafil, (6R ,12aS)-Tadalafil impurity A]; 1609405-34-6 (N-Ethyl tadalafil); 171596-36-4 (Nortadalafil, demethylated Tadalafil)

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    Molecular Weight (MW)389.4
    FormulaC22H19N3O4
    CAS No.171596-29-5 (Tadalafil); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 78 mg/mL (200.3 mM)
    Water: <1 mg/mL
    Ethanol: 50 mg/mL (145.6 mM)
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsC-351; IC 351; Tadalafil; IC351; Trade names: Adcirca, Cialis 

    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

    InChi Key: WOXKDUGGOYFFRN-IIBYNOLFSA-N

    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

    SMILES Code: O=C([[email protected]@]1([H])CC2=C([[email protected]@H](C3=CC(OCO4)=C4C=C3)N15)NC6=C2C=CC=C6)N(C)CC5=O           


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    In Vitro

    In vitro activity: Tadalafil binds to PDE5 with KD of 2.4 nM. cGMP stimulates the binding of [3H]Tadalafil. Tadalafil (1 mM) results increased CYP3A protein expression in human hepatocytes


    Kinase Assay: Biochemical potencies (affinities) of these compounds for PDE5 determined by IC(50), K(D) (isotherm), K(D) (dissociation rate), and K(D) ((1/2) EC(50)), respectively, were the following: 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). Thus, absolute potency values were similar for each inhibitor, and relative potencies were vardenafil >> tadalafil > sildenafil. 0.5 ml tadalafil solutions with different concentrations were added (0.2, 0.1, 0.05 and 0.025 μg ml-1, respectively) into semen samples. In both groups, samples treated with 0.2 μg ml-1 tadalafil had significant increase in sperm motility after 2 h incubation. 

    In VivoTadalafil (2 mg/kg) almost completely restores penile oxygenation and abolishes neurotomy induced increase and substantially rescues muscle/fiber ratio in penile sectionsin sham-operated rats. Tadalafil (2 mg/kg or 10 mg/kg) significantly improves neurological functional recovery and increases cerebral vascular density and the percentage of BrdU-positive endothelial cells around the ischemic boundary. Tadalafil selectively increases cGMP but not cAMP in brain of rats. Tadalafil decreases the number of apoptotic cells and increases the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice
    Animal modelSham-operated rats
    Formulation & DosageDissovled in saline; 2 mg/kg; oral gavage
    ReferencesMol Pharmacol. 2004 Jul;66(1):144-52; Clin Pharmacol Ther. 2005 Jan;77(1):63-75; J Sex Med. 2006 May;3(3):419-31.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Tadalafil


    Potency of inhibition of PDE catalytic activity by PDE5 inhibitors.




    Tadalafil

    Affinity of PDE5 for binding 3H inhibitors.  Mol Pharmacol. 2004 Jul;66(1):144-52.
     

    Tadalafil

    Effects of nucleotides and inhibitors on binding of 3H inhibitors to PDE5. Mol Pharmacol. 2004 Jul;66(1):144-52.




    Tadalafil

    Effect of cGMP on [3H]tadalafil binding.
     


    Tadalafil

    Dissociation of 3H inhibitors from PDE5 after infinite dilution. Mol Pharmacol.2004 Jul;66(1):144-52.


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