ICA-121431 is a nanomolar potent and broad-spectrumvoltage-gatedsodium channel(Na_v)blocker, shows equipotent selectivity for humanNa_v1.1andNa_v1.3subtypes withIC₅₀values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition ofNa_v1.2(IC₅₀=240 nM) and 1,000 fold selectivity againstNa_v1.4,Na_v1.6, and the TTX-resistant humanNa_v1.5andNa_v1.8channels (IC₅₀s >10 μM).

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_v1.5. 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^[1].
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^[1].
ICA-121431 is against hNa_vchannels 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 IC₅₀values of 0.1 μM, 0.37 μM, 1.1 μM, 1.3 μM, 1.9 μM, 11.6 μM, 0.032 μM, respectively^[1].
ICA-121431 is against hNa_vchannels 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 IC₅₀values 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^[1].

449.55

Solid

C₂₃H₁₉N₃O₃S₂

313254-51-2

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 44 mg/mL(97.88 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.56 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (5.56 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (5.56 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。