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Tadalafil

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Catalog No. T1398Cas No. 171596-29-5
Alias IC-351, Cialis

Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.

Tadalafil

Tadalafil

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Purity: 97.03%
Catalog No. T1398Alias IC-351, CialisCas No. 171596-29-5
Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$32In StockIn Stock
25 mg$50In StockIn Stock
50 mg$73In StockIn Stock
100 mg$112In StockIn Stock
500 mg$289In StockIn Stock
1 mL x 10 mM (in DMSO)$50In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:97.03%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.
Targets&IC50
PDE5:1.8 nM
In vitro
Tadalafil (at doses of 2 or 10 mg/kg) significantly promotes neural function recovery and increases both cerebral vascular density and the percentage of BrdU-positive endothelial cells. In rats undergoing sham surgery, Tadalafil (at a dose of 2 mg/kg) almost completely restored penile tissue oxygenation and countered the increase induced by nerve transection, while substantially enhancing the muscle/fiber ratio in certain penile tissue sections. When administered to the rat brain, Tadalafil selectively elevated cGMP levels rather than cyclic adenosine monophosphate. Furthermore, Tadalafil reduced the number of apoptotic cells in rats and increased the phosphorylation of kinase Akt and extracellular signal-regulated kinases 1/2 (two survival-related kinases).
In vivo
When acting on human hepatocytes, Tadalafil (1 mM) notably increases the expression of CYP3A proteins. Tadalafil can bind to type 5 phosphodiesterase (PDE5) with a dissociation constant (KD) of 2.4 nM, and this binding is stimulated by cyclic guanosine monophosphate (cGMP).
SynonymsIC-351, Cialis
Chemical Properties
Molecular Weight389.40
FormulaC22H19N3O4
Cas No.171596-29-5
SmilesO=C1N2[C@@H](C3=C(C=4C(N3)=CC=CC4)C[C@@]2(C(=O)N(C)C1)[H])C=5C=C6C(=CC5)OCO6
Relative Density.1.51 g/cm3
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 3.9 mg/mL (10.02 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5681 mL12.8403 mL25.6805 mL128.4027 mL
5 mM0.5136 mL2.5681 mL5.1361 mL25.6805 mL
10 mM0.2568 mL1.2840 mL2.5681 mL12.8403 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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