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ICA-121431

CAS No. : 313254-51-2

MCE 国际站：ICA-121431

产品活性：ICA-121431 是一种纳摩尔级别强效广谱电压门控钠通道 (Na_v) 阻滞剂，对人 Na_v1.1 和 Na_v1.3 亚型具有等效选择性，IC₅₀ 值分别为 13 nM 和 23 nM。ICA-121431 对Na_v1.2 的抑制作用较弱 (IC₅₀=240 nM)，对 Na_v1.4、Na_v1.6、抗TTX 的人 Na_v1.5、Na_v1.8 通道表现出大于 1000 倍的选择性(IC₅₀s >10 µM)。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

In Vitro: ICA-121431 interacts with human Na_v1.3 and the amino acid residues that may define selectivity for this channel over other related Na_v channels, including Na_v1.7 and Na_v 1.5. Data generated using conventional patch clamp electrophysiological recording using a pulse protocol whereby a 20-ms test pulse is preceded by an 8-s step to a voltage that inactivated half of the channels.
ICA-121431 is against Wild type hNa_v1.3 hNa_v1.5 hNa_v1.7 with IC₅₀s of 0.013 µM, >30 µM, 12 µM, respectively.
ICA-121431 is against hNa_v channels with point mutations,shows hNa_v1.3 M1 (S1510Y), hNa_v1.3 M2 (R1511W), hNa_v1.3 M3 (E1559D), hNa_v1.3 M1,3 (S1510Y/E1559D), hNa_v1.3 M2, 3 (R1511W/E1559D), hNa_v1.3 M1, 2, 3 (S1510Y/R1511W/E1559D), and hNa_v1.7 M1, 2, 3 (Y1537S/W1538R/D1586E) with IC₅₀ values of 0.1 µM, 0.37 µM, 1.1 µM, 1.3 µM, 1.9 µM, 11.6 µM, 0.032 µM, respectively.
ICA-121431 is against hNa_v channels with point mutations,shows hNa_v1.3/hNa_v1.5 S1-S4, hNa_v1.3/hNa_v1.5 S3-S4, hNa_v1.3/hNa_v1.5 S5-S6, hNa_v1.3/hNa_v1.7 S1, hNa_v1.3/hNa_v1.7 S2, hNa_v1.3/hNa_v1.7 S3-S4, and hNa_v1.3/hNa_v1.7 S5-S6 with IC₅₀ values of 0.083 µM, 1.2 µM, 11 µM, 2.0 µM, 0.045 µM, 0.030 µM, 0.30 µM, 1.0 µM, and 0.024 µM, respectively.

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