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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A127941-10mg | 10mg | In stock | $58.90 | |
A127941-50mg | 50mg | In stock | $226.90 |
Selective Na V 1.8 channel blocker
Synonyms | MFCD10574689 | 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furamide | AS-55982 | N-t-butoxycarbonyl-S-tritylcysteine | 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)- 2-furancarboxamide. | BCP9000209 | HMS3656L08 | EX-A083 | AB07953 | EC-000.2378 | SMR004702 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.Selective blocker of Na V 1.8 channels (IC 50 = 8 nM |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | CHANNEL BLOCKER |
Mechanism of action | Channel blocker of Na v1.8 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | A-803467 inhibits spontaneous and evoked action potentials in sensory neurons. It exhibits antinociceptive effects.A-803467 decreases the firing in spinal dorsal horn neurons in vivo. The small molecule A-803467 is a potent and selective Nav1.8 sodium channel blocker. Nav1.8 is a tetrodotoxin-resistant (TTX-R) sodium channel that contributes to pain sensation by transmitting pain stimuli in peripheral sensory neurons; blockage of this channel by A-803467 reduces pain with varying effectiveness in a number of different models.A-803467 has been used to further understand the role of Nav1.8 in transmitting pain stimuli and also can be used as an analgesic |
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IUPAC Name | 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide |
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INCHI | InChI=1S/C19H16ClNO4/c1-23-15-9-14(10-16(11-15)24-2)21-19(22)18-8-7-17(25-18)12-3-5-13(20)6-4-12/h3-11H,1-2H3,(H,21,22) |
InChi Key | VHKBTPQDHDSBSP-UHFFFAOYSA-N |
Canonical SMILES | COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC |
Isomeric SMILES | COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC |
WGK Germany | 3 |
PubChem CID | 16038374 |
Molecular Weight | 357.79 |
CAS Registry No. | 944261-79-4 |
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PubChem CID | 16038374 |
ChEMBL Ligand | CHEMBL250699 |
RCSB PDB Ligand | 95T, 95T |
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Solubility | DMSO 72 mg/mL Water <1 mg/mL Ethanol 11 mg/mL |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H302:Harmful if swallowed |
Precautionary Statements | P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |
WGK Germany | 3 |
1. Mohammed ZA et al.. (2020) An unbiased and efficient assessment of excitability of sensory neurons for analgesic drug discovery.. Pain, 161 (5): (1100-1108). [PMID:31929383] |
2. Ho WS et al.. (2013) Effective contractile response to voltage-gated Na+ channels revealed by a channel activator.. Am J Physiol Cell Physiol, 304 (8): (C739-47). [PMID:23364266] |
3. Yang F et al.. (2015) SDF1-CXCR4 signaling contributes to persistent pain and hypersensitivity via regulating excitability of primary nociceptive neurons: involvement of ERK-dependent Nav1.8 up-regulation.. J Neuroinflammation, 12 (219). [PMID:26597700] |
4. Ramachandra R et al.. (2012) Tetrodotoxin-resistant voltage-dependent sodium channels in identified muscle afferent neurons.. J Neurophysiol, 108 (8): (2230-41). [PMID:22855776] |