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Submit ReviewICA 121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). Exhibits up to 1,000 fold selectivity against other TTX-sensitive or resistant sodium channels (IC50 values are >10 μM for human NaV1.5 and NaV1.8 channels). Interacts with an inhibitory interaction site distinct from those bound by TTX and local anesthetic-like modulators.
ICA 121431 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 449.55 |
公式 | C23H19N3O3S2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 313254-51-2 |
PubChem ID | 998021 |
InChI Key | URSQNPPONHUJDL-UHFFFAOYSA-N |
Smiles | O=S(C1=CC=C(NC(C(C4=CC=CC=C4)C3=CC=CC=C3)=O)C=C1)(NC2=NC=CS2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 44.95 | 100 |
以下数据基于产品分子量 449.55。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.22 mL | 11.12 mL | 22.24 mL |
5 mM | 0.44 mL | 2.22 mL | 4.45 mL |
10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
参考文献是支持产品生物活性的出版物。
McCormack et al (2013) Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc.Natl.Acad.Sci. 110 2724 PMID: 23818614
If you know of a relevant reference for ICA 121431, please let us know.
关键词: ICA 121431, ICA 121431 supplier, Selective, NaV, blockers, Sodium, Channels, voltage-gated, voltage-dependent, Na+, ICA121431, Voltage-gated, 5066, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ICA 121431 的部分引用包括:
Darik A et al (2022) NaV1.1 is essential for proprioceptive signaling and motor behaviors. Elife 11 PMID: 36278870
Kocmalova et al (2017) Control of Neurotransmission by NaV1.7 in Human, Guinea Pig, and Mouse Airway Parasympathetic Nerves. J Pharmacol Exp Ther 361 172 PMID: 28138042
Ellen A et al (2019) Tetrodotoxin-Sensitive Sodium Channels Mediate Action Potential Firing and Excitability in Menthol-Sensitive Vglut3-Lineage Sensory Neurons. J Neurosci 39 7086-7101 PMID: 31300524
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