2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl)-phenyl]-acetamide Chemical Properties

Density 

1.409±0.06 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: soluble20mg/mL, clear

pka

7.03±0.10(Predicted)

form 

powder

color 

white to beige

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

InChIKey

URSQNPPONHUJDL-UHFFFAOYSA-N

Safety Information

Hazard Codes 

Xn

Risk Statements 

22-36

Safety Statements 

26

WGK Germany 

3

2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl)-phenyl]-acetamide Usage And Synthesis

Description

ICA 121431 is a voltage-gated sodium channel (Na_v) blocker that selectively blocks Na_v1.1 and Na_v1.3 over Na_v1.4, and Na_v1.5-1.8 channels (IC₅₀s = <20, 19, 240, and >10,000 nM, respectively). It induces a concentration-dependent hyperpolarizing shift in voltage dependence of inactivation of Na_v1.3 channels at a concentration 1 μM but has no effect on resting channels. Substitution of the Na_v1.3 domain IV voltage-sensor domain (VSD4) with the Na_v1.5 VSD4 reduces ICA 121431 potency by approximately 500-fold.

Uses

ICA 121431 is a voltage-gated sodium (Nav) channel inhibitor.

storage

+4°C

References

McCormack et al. (2013), Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels; Proc. Natl. Acad. Sci. USA 110 E2724 Ostenn et al. (2017), Pharmacology of the Nav1.1 domain IV voltage sensor reveals coupling between inactivation gating processes; Proc. Natl. Acad. Sci. USA 114 6836

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