Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-803467 is a selective NaV1.8 channel blocker.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 30.00 | |
10 mg | In stock | $ 47.00 | |
25 mg | In stock | $ 95.00 | |
50 mg | In stock | $ 189.00 | |
100 mg | In stock | $ 292.00 | |
200 mg | In stock | $ 409.00 | |
500 mg | In stock | $ 682.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 50.00 |
Description | A-803467 is a selective NaV1.8 channel blocker. |
Targets&IC50 | Nav1.8 channel:8 nM |
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. |
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. |
Synonyms | A 803467, A803467 |
Molecular Weight | 357.79 |
Formula | C19H16ClNO4 |
CAS No. | 944261-79-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 8.9 mg/mL (25 mM)
DMSO: 35.8 mg/mL (100 mM)
You can also refer to dose conversion for different animals. More
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A-803467 944261-79-4 Membrane transporter/Ion channel Sodium Channel inflammatory Inhibitor channel Nav1.8 Na channels neuropathic anti-nociception selective potent Na+ channels A 803467 sodium A803467 tetrodotoxin-resistant inhibit inhibitor