Tadalafil

SKU: orb1308738

Description

Tadalafil (IC-351) is a selective PDE5 inhibitor that prevents cGMP breakdown, leading to vascular smooth muscle relaxation. This mechanism supports research on erectile physiology and vascular function in both in vitro enzyme assays and in vivo models of blood flow and penile erection.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 171596-29-5
• MW: 389.40
• Purity: 97.03% (May vary between batches)
• Formula: C₂₂H₁₉N₃O₄
• SMILES: O=C1N2[C@@H](C3=C(C=4C(N3)=CC=CC4)C[C@@]2(C(=O)N(C)C1)[H])C=5C=C6C(=CC5)OCO6
• Target: PDE,Apoptosis
• Solubility: DMSO:3.9 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  PDE5:1.8 nM
• 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).
• 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).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IC351, IC-351, IC 351, Inhibitor, inhibit, Apoptosis, Cialis, Tadalafil, PDE5, Phosphodiesterase (PDE), phosphodiesterase

Compound Identifiers

PubChem CID

110635