1. Metabolic Enzyme/Protease
    Apoptosis
  2. Phosphodiesterase (PDE)
    Apoptosis
  3. Tadalafil

Tadalafil (Synonyms: IC-351)

Cat. No.: HY-90009A Purity: 99.93%
Handling Instructions

Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.

For research use only. We do not sell to patients.

Tadalafil Chemical Structure

Tadalafil Chemical Structure

CAS No. : 171596-29-5

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Based on 1 publication(s) in Google Scholar

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Description

Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.

IC50 & Target

IC50: 1.8±0.4nM (PDE 5)[1].

In Vitro

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[1]. 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[2].

In Vivo

The Tadalafil-treated group showed enhanced erectile function (intracavernosal pressure/mean arterial pressure) at 0.3, 0.5, 1, 3, and 5 Hz compared with diabetic group values at the respective frequencies that approached control values[3]. oral administration of tadalafil (20 mg) or sildenafil (100 mg) was given. In both groups, computer-assisted semen analysis parameters showed no significant difference. After the administration of tadalafil (2 h) and sildenafil (1 h), there was no significant difference observed in premature acrosome reaction incidence rate[2].

Clinical Trial
Molecular Weight

389.40

Formula

C₂₂H₁₉N₃O₄

CAS No.

171596-29-5

SMILES

O=C([[email protected]@]1([H])CC2=C([[email protected]@H](C3=CC=C(OCO4)C4=C3)N15)NC6=C2C=CC=C6)N(C)CC5=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 52 mg/mL (133.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

TadalafilIC-351IC351IC 351Phosphodiesterase (PDE)ApoptosisInhibitorinhibitorinhibit

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