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Tadalafil PDE inhibitor

Name: Tadalafil
Brand: Selleck Chemicals
SKU: S1512
Availability: InStock
Rating: 5 (20 reviews)

Cat.No.S1512

Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. This compound is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11

Chemical Structure

Molecular Weight: 389.4

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PDE Inhibitors	Rolipram IBMX (3-Isobutyl-1-methylxanthine) Icariin Mardepodect (PF-2545920) Cilomilast Deltarasin PF-8380 Enpp-1-IN-1 Ibudilast GSK256066

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (200.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.900mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 78 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	389.4	Formula	C₂₂H₁₉N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	171596-29-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	IC351			Smiles	CN1CC(=O)N2C(C1=O)CC3=C(C2C4=CC5=C(C=C4)OCO5)NC6=CC=CC=C36

Mechanism of Action

Features	Much more potent to PDE-5 than PDE-1 or PDE-6.
Targets/IC₅₀/Ki	PDE5 (Cell-free assay) 1.8 nM
In vitro	Tadalafil binds to PDE5 with K_D of 2.4 nM. cGMP stimulates the binding of [³H]this compound. This chemical (1 mM) results increased CYP3A protein expression in human hepatocytes.
In vivo	Tadalafil (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. This compound (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. It selectively increases cGMP but not cAMP in brain of rats. It 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15213306/ [2] https://pubmed.ncbi.nlm.nih.gov/15637532/ [3] https://pubmed.ncbi.nlm.nih.gov/16681467/ [4] https://pubmed.ncbi.nlm.nih.gov/16959227/ [5] https://pubmed.ncbi.nlm.nih.gov/18082193/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06290713	Not yet recruiting	Duchenne Muscular Dystrophy\|Duchenne Disease\|Muscular Dystrophy\|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

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Handling Instructions

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