Tadalafil | 99.97%(HPLC) | PDE inhibitor
Purity & Quality Control
Batch: Purity: 99.97%
Tadalafil Related Products
Signaling Pathway
Biological Activity
| Description | Tadalafil is a PDE-5 inhibitor with an IC50 value of 1.8 nM in a cell-free assay. This compound is known for its remarkable selectivity, being at least 9000 times more effective against PDE5 than against most other families of phosphodiesterases, with the notable exception of PDE11, which it can also partially inhibit. | ||
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| Features | Tadalafil demonstrates a significantly enhanced potency towards PDE-5 when compared to PDE-1 or PDE-6. | ||
| Targets |
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| In vitro | ||||
| In vitro | Tadalafil exhibits a binding affinity to PDE5 with a KD of 2.4 nM. The presence of cGMP facilitates increased binding of [3H]Tadalafil. [1] In human hepatocytes, Tadalafil (1 mM) leads to an increase in CYP3A protein expression. [2] | |||
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| In Vivo | ||
| In vivo | Administration of Tadalafil (2 mg/kg) nearly completely restores penile oxygenation while abolishing the increase induced by neurotomy, and it substantially enhances the muscle/fiber ratio in penile sections of sham-operated rats. [3] The drug (at dosages of 2 mg/kg or 10 mg/kg) is known to significantly enhance neurological functional recovery, augmenting cerebral vascular density as well as the percentage of BrdU-positive endothelial cells surrounding ischemic boundaries. Tadalafil also selectively boosts cGMP levels without affecting cAMP levels in the brains of rats. [4] Furthermore, Tadalafil reduces the number of apoptotic cells while elevating the phosphorylation of two survival-associated kinases: Akt and extracellular signal-regulated kinase 1/2 in mice. [5] | |
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| Animal Research | Animal Models | Sham-operated rats |
| Dosages | 2 mg/kg | |
| Administration | Orally | |
| 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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Chemical Information & Solubility
| Molecular Weight | 389.4 | 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) | |||
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In vitro |
DMSO: 78 mg/mL (200.3 mM) - Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO. Water: Insoluble Ethanol: Insoluble |
Molecular Weight Calculator |
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In vivo Add solvents to the product separately and in the specified order. |
In vivo Formulation Calculator |
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Preparing Stock Solutions
In vivo Formulation Calculator (Clear solution)
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Method for preparing DMSO master liquid: mg of 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 of DMSO master liquid, add μL of PEG300, mix thoroughly, then add μL of Tween 80, mix well, followed by μL of ddH2O, and mix again until clear.
Another method for preparing in vivo formulation: Take μL of DMSO master liquid, then add μL of Corn oil, mix thoroughly until a clear solution is formed.
Note: 1. Ensure the solution is clear before sequentially adding the next solvent.
2. Always follow the specified order for adding solvents. It is crucial to verify that the solution from the previous step is clear before proceeding with the next addition. You may use physical methods such as vortexing, ultrasound, or a hot water bath to assist with dissolving.
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