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Hlavní dokumenty

SML1964

Sigma-Aldrich

NS3728

≥98% (HPLC)

Synonyma:

1-[3,5-bis(Trifluoromethyl)phenyl]-3-[4-bromo-2-(1H-tetrazol-5-yl)phenyl]urea, Endovion, N-(3,5-bis(Trifluoromethyl)phenyl)-N′-(4-bromo-2-(1H-tetrazol-5-yl)phenyl)urea, NS 3728, NS-3728

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About This Item

Empirický vzorec (Hillův zápis):
C16H9BrF6N6O
Číslo CAS:
265646-85-3
Molekulová hmotnost:
495.18
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

SMILES string

FC(F)(F)c1cc(cc(c1)C(F)(F)F)NC(=O)Nc2c(ccc(c2)Br)c3n[nH]nn3

InChI

1S/C16H9BrF6N6O/c17-9-1-2-11(13-26-28-29-27-13)12(6-9)25-14(30)24-10-4-7(15(18,19)20)3-8(5-10)16(21,22)23/h1-6H,(H2,24,25,30)(H,26,27,28,29)

InChI key

OQRAKHDEGGGWQO-UHFFFAOYSA-N

Biochem/physiol Actions

A reversible anion channel blocker against VRAC (VSOAC) and CaCC channel anoctamin (ANO).
NS3728 (Endovion) is a di-aryl-urea-based reversible anion channel blocker that is shown to inhibit Ca(2+)-independent Cl- conductance by volume-regulated anion channel (VRAC or VSOAC; IC50 = 400 nM) as well as Ca2+-activated Cl- ccurrent (CaCC) by anoctamin (ANO) in an apparently voltage-dependent manner (IC50 against ANO1 = 2.1 and 0.7 μM at -95 and +50 mV, respectively). NS3728 is reported to be 5.5-times more potent than Tamoxifen against VRAC (IC50 = 0.4 vs. 2.2 μM).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

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Thomas Kjaer Klausen et al.
Journal of cellular physiology, 210(3), 831-842 (2006-11-18)
Recent evidence implicates the volume-regulated anion current (VRAC) and other anion currents in control or modulation of cell cycle progression; however, the precise involvement of anion channels in this process is unclear. Here, Cl- currents in Ehrlich Lettre Ascites (ELA)
N Hélix et al.
The Journal of membrane biology, 196(2), 83-94 (2004-01-16)
The endogenous volume-regulated anion channel (VRAC) from HEK293 cells was pharmacologically characterized using the whole-cell patch-clamp technique. Under isotonic conditions a small (1.3 nS), Ca(2+)-independent Cl conductance was measured. However, swelling at 75% tonicity activated a VRAC identified as an
Belinda Halling Sørensen et al.
American journal of physiology. Cell physiology, 310(11), C857-C873 (2016-03-18)
The leucine-rich repeat containing 8A (LRRC8A) protein is an essential component of the volume-sensitive organic anion channel (VSOAC), and using pharmacological anion channel inhibitors (NS3728, DIDS) and LRRC8A siRNA we have investigated its role in development of Cisplatin resistance in

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