| Name | A-740003 |
| Description | A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18/40 nM, for rat/human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice. |
| In vitro | A-438079 and A-740003 (10 μM) effectively inhibit the prolonged phase of BzATP-induced responses[1] and mitigate SE-induced TNF-α expression in dentate granule neurons while increasing SE-induced neuronal death[2]. 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 receptors[3]. Specifically, A-740003 robustly inhibits agonist-induced IL-1β release (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells[4]. |
| 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 (ED50=19 mg/kg i.p.), indicating its potency. Furthermore, A-740003 diminishes sensitivity to touch (tactile allodynia) in models of neuropathic pain, including chronic constriction of the sciatic nerve and vincristine-induced neuropathy. It also significantly lowers increased sensitivity to heat (thermal hyperalgesia) following the intraplantar introduction of carrageenan or complete Freund's adjuvant (ED50=38-54 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 9.5 mg/mL (20 mM)
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| Keywords | P2XRs | P2X Receptor | inhibit | Inhibitor | A-740003 | A740003 |
| Inhibitors Related | Opiranserin hydrochloride | Aurintricarboxylic acid | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | JNJ-55308942 | JNJ-42253432 | Ivermectin | Lappaconitine | CTP disodium dihydrate | Brilliant blue G-250 |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
