A-740003

SKU: orb1303893

Description

A-740003

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 861393-28-4
• MW: 474.55
• Purity: 99.68%
• Formula: C₂₆H₃₀N₆O₃
• SMILES: COc1ccc(CC(=O)NC(N\C(Nc2cccc3ncccc23)=N\C#N)C(C)(C)C)cc1OC
• Target: P2X Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.11 mM);DMSO:9.5 mg/mL (20.02 mM)

Bioactivity

• Target IC50:
  P2X7 (human):40 nM|P2X7 (rat):1 nM
• In Vivo:
  Administering A-740003 systemically results in a dose-dependent reduction of pain (antinociception) in rats, as evidenced in a spinal nerve ligation model (ED5 = 9 mg/kg i.p.), indicating its potency. furthermore , A-740003 diminishes sensitivity to touch (tactile allodynia) in models of neuropathic pain, including chronic constriction o the sciatic nerve and vincristine-induced neuropathy. It also significantly lowers increased sensitivity to heat (thermal hyperalgesia) followin the intraplantar introduction of carrageenan or complete Freund's adjuvant (ED5 = 8-54 mg/kg i.p.). however, A-740003 does not affect acute thermal pain in healthy rats and does not impair motor skills at doses that relieve pain.
• In Vitro:
  A-438079 and A-740003 (10 μM) effectively inhibi the prolonged phase of BzATP-induced response and mitigate SE-induced TNF-α expression in dentate granule neurons while increasing SE-induced neuronal deat. Compared to Other antagonists, both compounds exhibit superior efficacy in inhibiting P2X7 receptor activation across various species, with heightened activity in rat and human compared to mouse P2X7 receptor. Specifically, A-740003 robustly inhibits agonist-induced IL-1β release IC50 156 nM) and pore formation IC50 92 nM) in differentiated human THP-1 cell .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

A740003, A-740003, A 740003, inhibit, Inhibitor, P2X Receptor, P2X7 (Human), P2XRs, P2XReceptor, rat P2X7

Compound Identifiers

PubChem CID

72812793