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A-887826

Chemical Structure : A-887826

CAS No.: 1266212-81-0

A-887826 (A 887826)

Catalog No.: PC-49611Not For Human Use, Lab Use Only.

A-887826 (A 887826) is a potent and voltage-dependent Na(v)1.8 sodium channel blocker with IC50 of 11 nM (hNav1.8), potently blocks tetrodotoxin-resistant sodium (TTX-R Na(+)) currents (IC50=8 nM) from small diameter rat DRG neurons.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A-887826 (A 887826) is a potent and voltage-dependent Na(v)1.8 sodium channel blocker with IC50 of 11 nM (hNav1.8), potently blocks tetrodotoxin-resistant sodium (TTX-R Na(+)) currents (IC50=8 nM) from small diameter rat DRG neurons.
A-887826 is approximately 3 fold less potent to block Na(v)1.2, approximately 10 fold less potent to block tetrodotoxin-sensitive sodium (TTX-S Na(+)) currents and is >30 fold less potent to block Na(V)1.5 channels.
A-887826 effectively suppressed evoked action potential firing when DRG neurons were held at depolarized potentials and reversibly suppressed spontaneous firing in small diameter DRG neurons from complete Freund's adjuvant inflamed rats.
A-887826 significantly attenuated tactile allodynia in a rat neuropathic pain model.

Physicochemical Properties

M.Wt 480.99
Formula C26H29ClN4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(4-Butoxy-3-chlorophenyl)-N-[[2-(4-morpholinyl)-3-pyridinyl]methyl]-3-pyridinecarboxamide

References

1. Zhang XF, et al. Neuropharmacology. 2010 Sep;59(3):201-7.

2. Jo S, et al. Mol Pharmacol. 2023 Jan 12:MOLPHARM-AR-2022-000593.

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