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> Tadalafil [171596-29-5]

Tadalafil [171596-29-5]

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

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Tadalafil Chemical Structure

Tadalafil Chemical Structure

CAS No. : 171596-29-5

This product is a controlled substance and not for sale in your territory.

Based on 4 publication(s) in Google Scholar

Other Forms of Tadalafil:

  • Nortadalafil In-stock
  • cis-Tadalafil In-stock
  • ent-Tadalafil In-stock
  • cis-ent-Tadalafil In-stock
  • Tadalafil-d3 In-stock

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Voir toutes les isoformes

Description

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

IC50 & Target

PDE5

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tadalafil Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
Masse moléculaire

389.40

Formule

C22H19N3O4
CAS No.

171596-29-5
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1(21)CC2=C([C@@H](C3=CC=C(OCO4)C4=C3)N15)NC6=C2C=CC=C6)N(C)CC5=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : ≥ 52 mg/mL (133.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.92%

COA (263 KB) HNMR (287 KB) RP-HPLC (243 KB) LCMS (93 KB)

Instruction de manipulation (2659 KB)
Références

  • [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.  [Content Brief]

    [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]  [Content Brief]

    [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.  [Content Brief]

  • [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.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5681 mL 12.8403 mL 25.6805 mL 64.2013 mL
5 mM 0.5136 mL 2.5681 mL 5.1361 mL 12.8403 mL
10 mM 0.2568 mL 1.2840 mL 2.5681 mL 6.4201 mL
15 mM 0.1712 mL 0.8560 mL 1.7120 mL 4.2801 mL
20 mM 0.1284 mL 0.6420 mL 1.2840 mL 3.2101 mL
25 mM 0.1027 mL 0.5136 mL 1.0272 mL 2.5681 mL
30 mM 0.0856 mL 0.4280 mL 0.8560 mL 2.1400 mL
40 mM 0.0642 mL 0.3210 mL 0.6420 mL 1.6050 mL
50 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2840 mL
60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0700 mL
80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8025 mL
100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6420 mL
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Tadalafil Related Classifications

Help & FAQs

Keywords:

Tadalafil171596-29-5IC-351IC351IC 351Phosphodiesterase (PDE)ApoptosisInhibitorinhibitorinhibit

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