产品
编 号：F315670
分子式：C23H19N3O3S2
分子量：449.55
分子式：C23H19N3O3S2
分子量：449.55
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 313254-51-2
产品详情
生物活性：
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
体外研究：
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.
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
体外研究：
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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