Overview
Lyophilized Powder yes
Source Synthetic
MW: 449.5
Purity: >99%
Effective concentration 10 nM - 1 µM.
Structure
Chemical name 2,2-diphenyl-N-(4-(N-thiazol-2-ylsulfamoyl)phenyl) acetamide.
Molecular formula C23H19N3O3S2.
CAS No.: 313254-51-2
Activity ICA 121431 blocks NaV channels with IC50 values of 13 and 23 nM for NaV1.3 and NaV1.1 respectively1.
References-Activity
- McCormack, K. et al. (2013) Proc. Natl. Acad. Sci. U. S. A. 110, E2724.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Our bioassay
Alomone Labs ICA 121431 blocks NaV1. 3 channels expressed in Xenopus oocytes.A. Time course of NaV1.3 current amplitude and inhibition by 0.1 and 1 µM ICA 121431 (#I-170). Currents were elicited by application of a 50 ms voltage step to 0 mV, preceded by an inactivation inducing protocol (H.P= -120 mV, 1st step to 0 mV, 500 ms, recovering at -100 mV for 100 ms followed by the test step) , every 10 seconds. B. Superimposed example traces of current responses before and during perfusion of 0.1 and 1 µM ICA 121431, as indicated.
References - Scientific background
- McCormack, K. et al. (2013) Proc. Natl. Acad. Sci. U. S. A. 110, E2724.
Scientific background ICA 121431 is a synthetic potent and selective inhibitor of human NaV1.3 and NaV1.1 channels. ICA 121431 has an effective concentration of 10nM - 1μM with an IC50 of 13 and 23 nM on the NaV1.3 and NaV1.1 channels respectively. Unlike other known NaV inhibitors ICA inhibits the Nav channel by interacting with the S1-S4 voltage sensor segment of homologous domain 4. The sensitivity and selectivity of different NaV subtype receptors to ICA is influenced by the extracellular amino acid residues in the facing regions of the S2 and S3 transmembrane segments. Currently, most NaV modulators are unable to distinguish between NaV channel subtypes therefore limiting their usage due to systemic toxicity. ICA’s interaction with the region of the channel that controls voltage sensitivity enables subtype selective modulation and may be used as an efficient tool for innovative drug development1.
Target NaV1.1, NaV1.3 channels
Lyophilized Powder
ICA 121431 (#I-170) is a highly pure, synthetic, and biologically active compound.
Image & Title 
Alomone Labs ICA 121431 inhibits NaV1.3 channel in mouse primary small bowel EC cells.Representative Na+ currents elicited from small bowel EC cells by steps from -120 to -20 mV with increasing concentrations of ICA 121431 (#I-170), (left panel). Dose-response peak of Na+ currents to ICA 121431 concentrations (right panel).Adapted from Strege, P.R. et al. (2017) Sci. Rep. 7, 15650. with permission of SPRINGER NATURE.
For research purposes only, not for human use
Last Update: 07/05/2024
Applications
Citations
Citations
Powered by BiozProduct citations
- Strege, P.R. et al. (2017) Sci. Rep. 7, 15650.
