China Avanafil Supplier, Factories

Chemical Name:Avanafil CAS NO.:330784-47-9 Appearance:white to off-white powder Purpose:Treatment of male erectile dysfunction Assay:99%

Product Description

Overview

Avanafil is a highly selective phosphodiesterase type 5 (PDE5) inhibitor primarily used for the treatment of erectile dysfunction (ED). Known for its rapid onset and excellent receptor selectivity, Avanafil offers a favorable safety profile and reduced off-target effects compared to earlier PDE5 inhibitors in its class.

Chemical & Physical Properties

  • Purity: ≥ 99%
  • Appearance: White crystalline solid
  • Melting Point: 150–152 °C
  • Solubility:
    • Freely soluble in DMSO
    • Slightly soluble in 0.1 M HCl
    • Practically insoluble in water
  • LogP: Approx. 3.0
  • pKa: ~2 and 5.2

Pharmacological Profile

  • Target: PDE5
  • IC₅₀: ~5.2 nM (high potency)
  • Selectivity: Strong selectivity versus PDE1, PDE6, and PDE11
  • Onset of Action: ≈ 30–40 minutes
  • Half-Life: Approx. 1–1.5 hours
  • Elimination: Mainly excreted via bile and feces

Mechanism of Action

Avanafil selectively inhibits PDE5, blocking the degradation of cyclic guanosine monophosphate (cGMP) in smooth muscle cells. Increased cGMP levels promote vasodilation and enhanced blood flow in the corpus cavernosum, facilitating erection in the presence of sexual stimulation.

Applications

  • Pharmaceutical: Active pharmaceutical ingredient (API) used in oral ED formulations.
  • Research: Used in pharmacology, cardiovascular studies, and signaling pathway research involving cGMP/PDE5.

Key Advantages

  • Very high PDE5 selectivity
  • Faster onset than sildenafil or tadalafil
  • Reduced incidence of vision-related side effects
  • Suitable for rapid-acting ED formulations

Safety & Handling

  • Classified as an irritant; avoid inhalation and contact with eyes or skin.
  • Handle using standard laboratory protective equipment.
  • Store in a cool, dry, and well-sealed container.

Storage Conditions

  • Powder: Store at –20 °C, protected from moisture and light.
  • Solution (in DMSO): Store at –80 °C for long-term stability; avoid repeated freeze-thaw cycles.

Frequently Asked Questions (FAQ)

Q1: What is Avanafil and what is its primary application?
Avanafil is a highly selective phosphodiesterase type 5 (PDE5) inhibitor. It is mainly used as an Active Pharmaceutical Ingredient (API) for erectile dysfunction (ED) formulations and in cardiovascular/pharmacological research.
Q2: How fast does Avanafil act compared to other PDE5 inhibitors?
Avanafil has a rapid onset of action, typically working within 30 to 40 minutes, which is faster than earlier-generation inhibitors such as sildenafil or tadalafil.
Q3: What are the key advantages of Avanafil's pharmacological profile?
Avanafil offers high PDE5 selectivity over PDE1, PDE6, and PDE11, high potency (IC₅₀ ~5.2 nM), a rapid onset, and a reduced incidence of vision-related off-target side effects.
Q4: What is the solubility profile of Avanafil?
Avanafil is freely soluble in DMSO, slightly soluble in 0.1 M HCl, and practically insoluble in water.
Q5: How should Avanafil be stored to ensure stability?
In powder form, it should be stored at –20 °C protected from moisture and light. When dissolved in DMSO, it should be kept at –80 °C for long-term stability, avoiding repeated freeze-thaw cycles.
Q6: What safety precautions should be taken when handling Avanafil?
Since it is classified as an irritant, direct skin or eye contact and inhalation should be avoided. Standard protective equipment in a laboratory setting should always be used.

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