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Tadalafil | 99.97% (HPLC) | PDE Inhibitor

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Product Description

Catalog No.: S1512 Purity: 99.97%

Purity & Quality Control

Batch: Purity: 99.97%

Tadalafil Related Products

Signaling Pathway

Biological Activity

Description

Tadalafil is a PDE-5 inhibitor exhibiting an IC50 of 1.8 nM in a cell-free assay. This compound demonstrates over 9000-fold selectivity for PDE5 compared to other phosphodiesterase families, barring PDE11, which may experience partial inhibition.

Features

Significantly more potent against PDE-5 than against PDE-1 or PDE-6, showcasing its targeted action.

Targets

PDE5 ^[1]
(Cell-free assay)

1.8 nM

In vitro Analysis
In vitro Observations	Tadalafil binds to PDE5 with a K_D of 2.4 nM. The presence of cGMP enhances the binding of [³H]Tadalafil. ^[1] Notably, Tadalafil at a concentration of 1 mM escalates CYP3A protein expression in human hepatocytes. ^[2]

In Vivo Research
In vivo Effects	Administering Tadalafil at 2 mg/kg nearly restores penile oxygenation and offsets neurotomy-induced increases, significantly enhancing muscle/fiber ratios in penile tissues of sham-operated rats. ^[3] Further, doses of 2 mg/kg or 10 mg/kg of Tadalafil provide notable improvements in neurological recovery, enhancing cerebral vascular density and increasing the proportion of BrdU-positive endothelial cells in ischemic regions. This agent specifically elevates cGMP levels without influencing cAMP levels in the brains of rats. ^[4] Additionally, Tadalafil reduces apoptotic cell numbers and boosts the phosphorylation levels of survival-associated kinases, Akt and ERK1/2, in mouse models. ^[5]
Animal Research Details	Animal Models	Sham-operated rats
	Dosages	2 mg/kg
	Administration Method	Orally

NCT Number	Recruitment Status	Conditions Being Studied	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from ClinicalTrials.gov, updated on 2024-05-22)
NCT06290713	Not yet recruiting	Duchenne Muscular Dystrophy\|Duchenne Disease\|Muscular Dystrophy in Children\|Vasodilation\|Exercise\|DMD	University of Florida\|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)	March 2024	Phase 2
NCT05884957	Completed	Erectile Dysfunction\|Diabetes Mellitus	Egymedicalpedia	June 1, 2023	Not Applicable
NCT05709574	Recruiting	Gastric Adenocarcinoma\|Gastroesophageal Junction Adenocarcinoma	University of Arizona	April 20, 2023	Phase 2
NCT05466695	Not yet recruiting	Erectile Dysfunction and Neutrophil Lymphocyte Ratio	Assiut University	August 1, 2022	Early Phase 1
NCT05173896	Recruiting	Cerebral Small Vessel Diseases\|Stroke Ischemic	Christina Kruuse\|Danish Research Centre for Magnetic Resonance\|Bispebjerg Hospital\|Rigshospitalet Denmark\|Hillerod Hospital Denmark\|University of Copenhagen\|The Novo Nordic Foundation\|Herlev Hospital	May 31, 2022	Phase 2

References
[1] Blount MA, et al. Mol Pharmacol, 2004, 66(1), 144-152. [2] Ring BJ, et al. Clin Pharmacol Ther, 2005, 77(1), 63-75. [3] Vignozzi L, et al. J Sex Med, 2006, 3(3), 419-431. [4] Zhang L, et al. Brain Res, 2006, 1118(1), 192-198. [5] Lysiak JJ, et al. J Urol, 2008, 179(2), 779-785. + Expand

References

[1] Blount MA, et al. Mol Pharmacol, 2004, 66(1), 144-152.
[2] Ring BJ, et al. Clin Pharmacol Ther, 2005, 77(1), 63-75.
[3] Vignozzi L, et al. J Sex Med, 2006, 3(3), 419-431.

[4] Zhang L, et al. Brain Res, 2006, 1118(1), 192-198.
[5] Lysiak JJ, et al. J Urol, 2008, 179(2), 779-785.

+ Expand

Chemical Information & Solubility

Molecular Weight	389.4	Chemical Formula	C₂₂H₁₉N₃O₄
CAS No.	171596-29-5	SDF	Download Tadalafil SDF
Smiles	CN1CC(=O)N2C(C1=O)CC3=C(C2C4=CC5=C(C=C4)OCO5)NC6=CC=CC=C36
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to prevent repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO: 78 mg/mL (200.3 mM) - Note that moisture-absorbing DMSO reduces solubility; always use fresh DMSO.

Water: Insoluble

Ethanol: Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product stepwise and in the specified order.

In vivo Formulation Calculator

Preparing Stock Solutions

In vivo Formulation Calculator (for clear solutions)

Step 1: Enter the required data below (It is recommended to use an additional animal to account for experimental loss).

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Specify the in vivo formulation (This is a calculator only; please contact us first if there is no in vivo formulation provided in the solubility section.).

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Preparation method for DMSO master liquid: mg of drug pre-dissolved in μL DMSO (ensure master liquid concentration does not exceed solubility limits of the current batch).

Method for preparing in vivo formulation: Take μL DMSO master liquid, follow with μL PEG300, mix well, then add μL Tween 80, mix again, and finally add μL ddH₂O, mixing thoroughly.

Another method for in vivo formulation: Take μL DMSO master liquid, followed by μL Corn oil, mix thoroughly.

Note: 1. Ensure that each liquid remains clear prior to adding subsequent solvents.
2. Always introduce solvents in order, confirming that each resultant solution remains clear before proceeding to the next addition. Utilize vortexing, ultrasound, or hot water baths as necessary to aid in dissolution.