1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

Tadalafil 

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

Tadalafil 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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10 mM * 1 mL in DMSO USD 92 In-stock
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Description

Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8 nM. IC50 Value: 1.8±0.4nM [1] Target: PDE 5 Tadalafil is marketed in pill form for treating erectile dysfunction(ED) under the name Cialis, and under the name Adcirca for the treatment of pulmonary arterial hypertension. Tadalafil can elevate the level of cGMP in the corpus cavernosum and effectively improve ED of various causes and degrees. 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 (P <.05) 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: Study the Safety and Effectiveness of Tadalafil in Men With Problems Getting or Maintaining an Erection When Taken Prior to Desiring an Erection. Phase 3

Clinical Trial
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
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Tadalafil
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Tadalafil

Cat. No.: HY-90009A