2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. ICA-121431

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).

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ICA-121431 Chemical Structure

ICA-121431 Chemical Structure

CAS No. : 313254-51-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 85 In-stock
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid
5 mg USD 78 In-stock
10 mg USD 125 In-stock
50 mg USD 370 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

ICA-121431 Related Antibodies

Top Publications Citing Use of Products

View All Sodium Channel Isoform Specific Products:

View All Isoforms
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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).

IC50 & Target[1]

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)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
< 20 nM
Compound: 16, ICA-121431
Inhibition of human TTX-sensitive NaV1.3 channel expressed in HEK293 cells by patch clamp electrophysiology assay
Inhibition of human TTX-sensitive NaV1.3 channel expressed in HEK293 cells by patch clamp electrophysiology assay
[PMID: 25927480]
HEK293 IC50
> 10 μM
Compound: 16, ICA-121431
Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay
Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay
[PMID: 25927480]
HEK293 IC50
> 10 μM
Compound: 16, ICA-121431
Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay
Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay
[PMID: 25927480]
In Vitro

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[1].
ICA-121431 is against Wild type hNav1.3 hNav1.5 hNav1.7 with IC50s of 0.013 μM, >30 μM, 12 μM, respectively[1].
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[1].
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ICA-121431 Related Antibodies
Molecular Weight

449.55

Formula

C23H19N3O3S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(S(NC2=NC=CS2)(=O)=O)C=C1)C(C3=CC=CC=C3)C4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (97.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2244 mL 11.1222 mL 22.2445 mL
5 mM 0.4449 mL 2.2244 mL 4.4489 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2244 mL 11.1222 mL 22.2445 mL 55.6112 mL
5 mM 0.4449 mL 2.2244 mL 4.4489 mL 11.1222 mL
10 mM 0.2224 mL 1.1122 mL 2.2244 mL 5.5611 mL
15 mM 0.1483 mL 0.7415 mL 1.4830 mL 3.7074 mL
20 mM 0.1112 mL 0.5561 mL 1.1122 mL 2.7806 mL
25 mM 0.0890 mL 0.4449 mL 0.8898 mL 2.2244 mL
30 mM 0.0741 mL 0.3707 mL 0.7415 mL 1.8537 mL
40 mM 0.0556 mL 0.2781 mL 0.5561 mL 1.3903 mL
50 mM 0.0445 mL 0.2224 mL 0.4449 mL 1.1122 mL
60 mM 0.0371 mL 0.1854 mL 0.3707 mL 0.9269 mL
80 mM 0.0278 mL 0.1390 mL 0.2781 mL 0.6951 mL
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ICA-121431 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ICA-121431313254-51-2ICA121431ICA 121431Sodium ChannelNa channelsNa+ channelsNavchannelinhibitorTTX-resistantInhibitorinhibit

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