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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-A-887826
A-887826

Chemical Structure : A-887826

CAS No.: 1266212-81-0

A-887826 (A 887826)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 480.99
分子式 C26H29ClN4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

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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