A-803467 NEW
| Price | $29 | $57 | $113 |
| Package | 10mg | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: A-803467 | CAS No.: 944261-79-4 |
| Purity: 98% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | A-803467 |
| Description | A-803467 is a selective NaV1.8 channel blocker. |
| Kinase Assay | Maize HD2, HD1-B, and HD1-A Enzyme Inhibition.: The enzyme liberats tritiated acetic acid from the substrate, which is quantified by scintillation counting. IC50 values are results of triple determinations. A 50 μL sample of maize enzyme (at 30 °C) is incubated (30 min) with 10 μL of total [3H]acetate-prelabeled chicken reticulocyte histones (2 mg/mL). Reaction is stopped by addition of 50 μL of 1 M HCl/0.4 M acetate and 800 μL of ethyl acetate. After centrifugation (1×104 g, 5 min), an aliquot of 600 μL of the upper phase is counted for radioactivity in 3 mL of liquid scintillation cocktail. MC1568 is tested at a starting concentration of 40 μM, and active substances are diluted further. NaB, VPA, TSA, SAHA, 85 TPX, HC-toxin, and tubacin are used as the reference compounds, and blank solvents are used as negative controls. |
| In vitro | A-803467 effectively reduced pain sensitivity in a dose-dependent manner in models including spinal nerve ligation (ED50 = 47 mg/kg, ip), sciatic nerve injury (ED50 = 85 mg/kg, ip), capsaicin-induced secondary mechanical allodynia (ED50 ≈ 100 mg/kg, intraperitoneally), and hyperalgesia following complete Freund's adjuvant injection into the plantar foot (ED50 = 41 mg/kg, intraperitoneally). Consistent with its effects on neuronal action potentials in vitro, systemic administration of A-803467 (20 mg/kg, iv) to rats with spinal nerve ligation significantly reduced both spontaneous and von Frey hair-induced responses in wide dynamic range neurons of the spinal cord dorsal horn by 66% and 53%, respectively. However, A-803467 was ineffective in models of harm induced by formalin, as well as acute thermal, postoperative pain, and pain caused by chemotherapy (vincristine). |
| In vivo | A-803467 selectively blocks tetrodotoxin-resistant (TTX-R) currents in rat dorsal root ganglion neurons in a concentration-dependent manner, with an IC50 of 140 nM, proving more effective than mexiletine and lamotrigine (IC50> 30 μM). It exhibits 300 to 1,000 times higher selectivity for hNaV1.8 over hNaV1.2, hNaV1.3, hNaV1.5, and hNaV1.7 channels, with respective IC50 values of 7.38 μM, 2.45 μM, 7.34 μM, and 6.74 μM. A-803467 shows no significant activity against other channels and receptors expressed in peripheral sensory neurons (including TRPV1, P2X2/3, CaV2.2, and KCNQ2/3 channels), with an IC50 > 10 μM. It effectively blocks recombinant human or rat Nav1.8 channels at IC50s of 8 nM and 45 nM, maintained at a -40 mV potential. A-803467 also blocks human NaV1.8 channels in a resting state, with an IC50 of 79 nM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 8.9 mg/mL (25 mM) DMSO : 65 mg/mL (181.67 mM) |
| Keywords | Sodium Channel | inflammatory | Inhibitor | channel | Nav1.8 | Na channels | neuropathic | anti-nociception | selective | potent | Na+ channels | sodium | tetrodotoxin-resistant | A-803467 | inhibit |
| Inhibitors Related | Phenytoin sodium | Lidocaine Hydrochloride hydrate | Lidocaine | Valproic Acid | Butamben | Lidocaine hydrochloride | L-Aspartic aicd sodium | Mebeverine hydrochloride | Amitriptyline hydrochloride | Riluzole | Benzocaine | Nefopam hydrochloride |
| Related Compound Libraries | Highly Selective Inhibitor Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted 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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