Home Transmembrane Transporters Sodium Channel inhibitor A-803467 For research use only.

A-803467

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

A-803467 Chemical Structure

A-803467 Chemical Structure

CAS: 944261-79-4

Selleck's A-803467 has been cited by 2 publications

Purity & Quality Control

Batch: S278501 DMSO] 72 mg/mL] false] Ethanol] 11 mg/mL] false] Water] Insoluble] false Purity: 99.45%
99.45

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Signaling Pathway

Sodium Channel Signaling Pathways

Sodium Channel Signaling Pathway

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Biological Activity

Description A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.
Features The 1st small-molecule blocker of sodium channels showing both high potency and significant subtype-selectivity among the sodium channel family.
Targets
Na(V1.8) channel [1]
8 nM
In vitro
In vitro A-803467 potently blocks recombinant human or rat NaV1.8 channels with IC50 of 8 nM and 45 nM, respectively, at a holding potential of -40 mV. At a resting state, A-803467 also potently blocks human NaV1.8 channels with IC50 of 79 nM. A-803467 blocks tetrodotoxin-resistant (TTX-R) currents in rat dorsal root ganglion neurons in a concentration-dependent manner with IC50 of 140 nM, more potently compared with both mexiletine and lamotrigine with IC50 of >30 μM. A-803467 displays 300- to 1,000-fold higher selectivity for hNaV1.8 over hNaV1.2, hNaV1.3, hNaV1.5, and hNaV1.7 channels with IC50 of 7.38 μM, 2.45 μM, 7.34 μM, and 6.74 μM, respectively. 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 IC50 >10 μM. A-803467 also shows no or weak activity against a broad screening panel of cell-surface receptors, ion channels, and enzymes with IC50 of >2 μM. A-803467 at 0.3 μM but not 0.1 μM significantly inhibits the generation of spontaneous and electrically evoked action potentials. [1]
Experimental Result Images Methods Biomarkers Images PMID
Western blot HERC2 / USP33 / USP20 24855649
In Vivo
In vivo Consistent with its effects on neuronal action potential electrogenesis in vitro, systemic administration of A-803467 (20 mg/kg, i.v.) to spinal nerve ligated rats, significantly reduces both spontaneous and von Frey hairevoked firing of spinal dorsal horn wide dynamic range neurons by 66% and 53%, respectively, compared with baseline levels. Administration of A-803467 also dose-dependently reduces mechanical allodynia in a variety of rat pain models including spinal nerve ligation (ED50 = 47 mg/kg, i.p.), sciatic nerve injury (ED50 = 85 mg/kg, i.p.), capsaicin-induced secondary mechanical allodynia (ED50 ≈ 100 mg/kg, i.p.), and thermal hyperalgesia after intraplantar complete Freund's adjuvant injection (ED50 = 41 mg/kg, i.p.). A-803467 is inactive against formalin-induced nociception and acute thermal and postoperative pain, as well as in a chemotherapy-induced pain model (vincristine). [1]
Animal Research Animal Models Male Sprague–Dawley rats subjected to spinal nerve ligation, sciatic nerve injury, capsaicin-induced secondary mechanical allodynia, or thermal hyperalgesia after intraplantar complete Freund's adjuvant injection, and male CD1 mice subjected to the abdomi
Dosages ~100 mg/kg
Administration Injected i.p. 30 minutes before behavioral testing

Chemical Information & Solubility

Molecular Weight 357.79 Formula

C19H16ClNO4
CAS No. 944261-79-4 SDF Download A-803467 SDF
Smiles COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (201.23 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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