品牌	貨號	產品規格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S84879-10mg	98%	￥750.00元	9	-	-	-
源葉(MedMol)	S84879-50mg	98%	￥2200.00元	8	-	-	-
源葉(MedMol)	S84879-250mg	98%	￥5800.00元	2	-	-	-

產品介紹

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)

產品描述： 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)

靶點： hNav1.1:13 nM (IC50);hNav1.3:23 nM (IC50);hNav1.4:240 nM (IC50);hNav1.6:>10 μM (IC50);hNav1.5:>10 μM (IC50);hNav1.8:>10 μM (IC50);SodiumChannel

體外研究：
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 against hNav 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 against hNav 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

參考文獻：
1. McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels.Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32.

溶解性： Soluble in DMSO

保存條件： -20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.224 ml	11.122 ml	22.245 ml
5 mM	0.445 ml	2.224 ml	4.449 ml
10 mM	0.222 ml	1.112 ml	2.224 ml
50 mM	0.044 ml	0.222 ml	0.445 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

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ICA-121431 98%

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