Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 8,000 | |||
10 mg | 在庫あり | ¥ 12,500 | |||
50 mg | 在庫あり | ¥ 16,500 | |||
100 mg | 在庫あり | ¥ 26,500 |
説明 | 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. |
ターゲット&IC50 | P2X7 (rat):18nM, P2X7 (human):40 nM |
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. |
別名 | A 740003 |
分子量 | 474.55 |
分子式 | C26H30N6O3 |
CAS No. | 861393-28-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9.5 mg/mL(20 mM)
You can also refer to dose conversion for different animals. 詳細
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A-740003 861393-28-4 Membrane transporter/Ion channel Neuroscience P2X Receptor P2XRs inhibit A 740003 Inhibitor A740003 inhibitor