ICA-121431
Based on 4 publication(s) in Google Scholar
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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.35%
- CAS No.: 313254-51-2
- 화학식: C23H19N3O3S2
- 분자량:449.55
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ICA-121431
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Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
<20 nM
Compound: 16, ICA-121431
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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
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[PMID: 25927480] |
| HEK293 | IC50 |
>10 μM
Compound: 16, ICA-121431
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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
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[PMID: 25927480] |
| HEK293 | IC50 |
>10 μM
Compound: 16, ICA-121431
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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
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[PMID: 25927480] |
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.
Chemical Information
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CAS No. 313254-51-2
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Appearance Solid
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분자량 449.55
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화학식 C23H19N3O3S2
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Color White to off-white
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SMILES
O=C(NC1=CC=C(S(NC2=NC=CS2)(=O)=O)C=C1)C(C3=CC=CC=C3)C4=CC=CC=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Acta Biomater
2022 Oct 15:152:255-272. PMID: 36041647 -
PLoS Biol
Amyloid precursor protein modulates cerebellar Purkinje cell activity and motor function through regulation of Nav1.6 currents. [Abstract]2025 Nov 24;23(11):e3003513. PMID: 41284713 -
Commun Biol
Permethrin induces epileptic susceptibility via activation of Na+ channels and rise in glutamate. [Abstract]2025 Nov 24;8(1):1644. PMID: 41286411 -
iScience
Nuclear Factor-kappaB Gates Nav1.7 Channels in DRG Neurons via Protein-Protein Interaction. [Abstract]2019 Sep 27:19:623-633. PMID: 31446225
용액&용해도
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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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