A-740003 NEW
| Price | $34 | $53 | $72 |
| Package | 5mg | 10mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-05-02 |
Product Details
| Product Name: A-740003 | CAS No.: 861393-28-4 |
| Purity: 99.68% | Supply Ability: 10g |
| Release date: 2025/05/02 |
Product Introduction
Bioactivity
| 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 (20.02 mM), Sonication is recommended. |
| Keywords | rat P2X7 | P2XRs | P2XReceptor | P2X7 (Human) | P2X Receptor | Inhibitor | inhibit | A-740003 | A740003 |
| Inhibitors Related | Gefapixant citrate | Opiranserin hydrochloride | Aurintricarboxylic acid | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | 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 | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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