AF 353

SKU: orb1223815

Description

AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).

Key Properties

• CAS Number: 865305-30-2
• MW: 400.21
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₇IN₄O₂
• SMILES: NC1=NC=C(OC2=CC(I)=C(OC)C=C2C(C)C)C(N)=N1
• Target: P2 Receptor
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  AF-353 (Ro-4) does not compromise oxygen levels or cardiac function. AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i. v. ; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats. AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i. v. ; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced. Animal model: Female Sprague-Dawley rats (250–300 g) bearing SCI. Dosage: 10 mg/kg, 20 mg/kg. Administration: Intravenous injection; interval of 90 minutes, for 4 hours to 6 hours. Result: Significantly reduced purinergic response in both normal and SCI rats.
• In Vitro:
  AF-353 (Ro-4) is a highly potent inhibitor of α, β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 (Ro-4) also blocks human P2X2/3 channel function with marginally reduced potency with a p50 of 7.3.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ro-4

Quick Database Links

Gene Symbol

P2 Receptor