ICA-121431

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ICA-121431 是一种纳摩尔级强效小分子 Nav1.7 通道抑制剂，对大鼠 Nav1.7 的 IC50 为 19 nM，对人 Nav1.5 或 Nav1.7 通道几乎没有或没有活性。

ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7 with little or no activity against human Nav1.5 or Nav1.7 channels.

ICA-121431 interacts with human Nav1.3 and the amino acid residues that may define selectivity for this channel over other related Nav?channels, including Nav1.7 and Nav 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 hNav1.3 hNav1.5 hNav1.7 with IC50s of 0.013 μM, >30 μM, 12 μM, respectively.ICA-121431 is againsthNav channels with point mutations,shows hNav1.3 M1 (S1510Y), hNav1.3 M2 (R1511W), hNav1.3 M3 (E1559D), hNav1.3 M1,3 (S1510Y/E1559D), hNav1.3 M2, 3 (R1511W/E1559D), hNav1.3 M1, 2, 3 (S1510Y/R1511W/E1559D), and hNav1.7 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 againsthNav channels with point mutations,shows hNav1.3/hNav1.5 S1-S4, hNav1.3/hNav1.5 S3-S4, hNav1.3/hNav1.5 S5-S6, hNav1.3/hNav1.7 S1, hNav1.3/hNav1.7 S2, hNav1.3/hNav1.7 S3-S4, and hNav1.3/hNav1.7 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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22-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl

Membrane Transporter/Ion Channel

Sodium Channel

Nav1.7 channel

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313254-51-2

449.55

C23H19N3O3S2

>98% (HPLC)

DMSO:44 mg/mL (97.88 mM)

O=C(Nc1ccc(cc1)S(=O)(=O)Nc1nccs1)C(c1ccccc1)c1ccccc1

22-diphenyl-N-(4-(N-(thiazol-2-yl)sulfamoyl)phenyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years