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ICA-121431

Name: ICA-121431
Brand: TargetMol
SKU: T7336
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7336Cas No. 313254-51-2

Alias 2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

ICA-121431

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Purity: 98.06%

Catalog No. T7336Alias 2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoylCas No. 313254-51-2

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$40	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$90	In Stock	In Stock
25 mg	$158	In Stock	In Stock
50 mg	$265	In Stock	In Stock
100 mg	$398	-	In Stock
1 mL x 10 mM (in DMSO)	$68	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.06%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

ICA-121431 AI Summary

ICA-121431 inhibits various sodium channels as indicated by its IC50 values. It shows relatively weak inhibition for NaV1.7, NaV1.8, NaV1.6, NaV1.5, and NaV1.4 channels (IC50 > 10000.0 nM), but is more potent against NaV1.2 and NaV1.1 channels with IC50 values of 240.0 nM and < 20.0 nM, respectively. It also demonstrates selectivity for the NaV1.5 channel with selectivity ratios of 1000.0 compared to NaV1.7, NaV1.6, NaV1.3, and NaV1.1. Additionally, it shows moderate to low inhibitory activity on other sodium channels like NaV1.3, with selectivity in its inhibition profile. ICA-121431 exhibits antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, with inhibition values ranging from -0.91% to 0.19% at 10 uM after 48 hours. It also inhibits the SARS-CoV-2 3CL-Pro protease at 20 µM, showing FRET response-based inhibition of 10.07% and 21.53%. Additionally, it inhibits human HDAC6 enzyme activity (60.63% with commercial and 1.03% with custom peptide substrates). The compound shows varying effects on cell viability: moderate to high impact on HEK293T cells (growth rates 0.52 to 0.94), moderate impact on U2OS cells (0.81 to 0.94), and significant inhibitory effect on human fibroblast cells (-0.85 growth rate). It also demonstrates good aqueous solubility, moderate hepatic clearance, significant inhibition of CYP2C9 activity, high efflux ratio across RRCK cells expressing MDR1, and moderate lipophilicity. Overall, ICA-121431 demonstrates diverse bioactivity, including potent sodium channel inhibition, antiviral properties against SARS-CoV-2, HDAC6 inhibition, and varying effects on cell viability, making it a versatile candidate for further research..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.
Targets&IC50	Nav1.7:19 nM, Nav1.5 (human):>10 μM, Nav1.4 (human):240 nM, Nav1.3 (human):23 nM, Nav1.6 (human):>10 μM, Nav1.1 (human):13 nM, Nav1.8 (human):>10 μM
Synonyms	2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl

Chemical Properties

Molecular Weight	449.55
Formula	C₂₃H₁₉N₃O₃S₂
Cas No.	313254-51-2
Smiles	O=C(Nc1ccc(cc1)S(=O)(=O)Nc1nccs1)C(c1ccccc1)c1ccccc1
Relative Density.	1.409 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 110 mg/mL (244.69 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.45 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2244 mL	11.1222 mL	22.2445 mL	111.2223 mL
5 mM	0.4449 mL	2.2244 mL	4.4489 mL	22.2445 mL
10 mM	0.2224 mL	1.1122 mL	2.2244 mL	11.1222 mL
20 mM	0.1112 mL	0.5561 mL	1.1122 mL	5.5611 mL
50 mM	0.0445 mL	0.2224 mL	0.4449 mL	2.2244 mL
100 mM	0.0222 mL	0.1112 mL	0.2224 mL	1.1122 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc