A-740003
Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy-
CAS: 861393-28-4
Molecular Formula: C26H30N6O3
A-740003 - Names and Identifiers
A-740003 - Physico-chemical Properties
| Molecular Formula | C26H30N6O3 |
| Molar Mass | 474.55 |
| Density | 1.19±0.1 g/cm3(Predicted) |
| Melting Point | 128-129 °C |
| Solubility | DMSO: soluble10mg/mL, clear (warmed) |
| Appearance | powder |
| Color | white to light brown |
| pKa | 14.09±0.46(Predicted) |
| Storage Condition | 2-8°C |
| MDL | MFCD09970333 |
| Use | A- 740003 is a selective inhibitor of P2X7 receptor, and its IC50 for mouse and human P2X7 receptor is 18 and 40 nM respectively. |
| In vitro study | A 438079 or A 740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death. A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A-740003 and A-438079 show greater activity at rat and human, as compared with mouse P2X7 receptors. A-740003 potently blocks agonist-evoked IL-1β release with (IC 50 =156 nM) and pore formation (IC 50 =92 nM) in differentiated human THP-1 cells. |
| In vivo study | Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED 50 =19 mg/kg i.p.) in the rat. A-740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED 50 =38-54 mg/kg i.p.). A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses. |
A-740003 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
A-740003 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.107 ml | 10.536 ml | 21.073 ml |
| 5 mM | 0.421 ml | 2.107 ml | 4.215 ml |
| 10 mM | 0.211 ml | 1.054 ml | 2.107 ml |
| 5 mM | 0.042 ml | 0.211 ml | 0.421 ml |
Last Update：2024-01-02 23:10:35
A-740003 - Reference Information
| biological activity | A-740003 is an effective and selective competitive antagonist of P2X7 receptor. the IC50 values of P2X7 receptors in rats and humans are 18 nM and 40 nM respectively. A- 740003 can effectively block agonist-induced IL-1β release and pore formation in differentiated human THP-1 cells, with corresponding IC50 values of 156 nM and 92 nM respectively. |
| target | TargetValue rat P2X7 receptor 18 nM human P2X7 receptor 40 nM IL-1β pore formation 92 nM IL-1β release 156 nM |
| Target | Value |
| rat P2X7 receptor (Cell-free assay) | 18 nM |
| human P2X7 receptor (Cell-free assay) | 40 nM |
| IL-1β pore formation (Cell-based assay) | 92 nM |
| IL-1β release (Cell-based assay) | 156 nM |
| in vitro study | A 438079 or A 740003 (10 μ M) significantly blocks the sustained phase of the BzATP-induced response. A- 740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A- 740003 infusions increases SE-induced neuronal death. A- 740003 and A- 438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A- 740003 and A- 438079 show greater activity at rat and human, as compared with mouse P2X7 receptors. A- 740003 potently blocks agonist-evoked IL-1β release with (IC 50=156 nM) and pore formation (IC 50=92 nM) in differentiated human THP-1 cells. |
| in vivo study | Systemic administration of A- 740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED 50=19 mg/kg I. p.) in the rat. A- 740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A- 740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED 50 = 38-54mg/kg I. p.). A- 740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses. |
Last Update：2024-04-09 21:11:58
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Product Name: A-740003 Visit Supplier Webpage Request for quotationCAS: 861393-28-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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