GLPBio

SN-6

Catalog No.: GC15195Purity:>99.50%
Na+/Ca2+ exchange inhibitor

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SN-6
Cas No.: 415697-08-4
10mM (in 1mL DMSO)In Stock
$67.00
1
1mgIn Stock
$33.00
1
5mgIn Stock
$75.00
1
10mgIn Stock
$117.00
1
25mgIn Stock
$234.00
1
50mgIn Stock
$350.00
1
100mgIn Stock
$504.00
1

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Description

SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, and inhibits 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.

SN 6 is a selective Na+/Ca2+ exchanger inhibitor, which inhibits the initial rate of 45Ca2+ uptake into NCX1, NCX2, and NCX3 transfectants with IC50 values of 2.9 ± 0.12, 16 ± 1.1, and 8.6 ± 0.27 μM. SN 6 (up to 30 μM) also less potently inhibits muscarinic acetylcholine receptor, with a higher IC50 of 18 μM. SN 6 (0.3-30 μM) completely inhibits the initial rate of Na+i-dependent 45Ca2+ uptake into Na+-loaded sarcolemmal vesicles in a dose dependent manner (IC50, 5.3 ± 0.37 μM). SN 6 (0.3-10 μM) dose-dependently protects against the hypoxia/reoxygenation-induced LDH release in parental LLC-PK1 cells and NCX1 transfectants but not in K229Q transfectants[1]. SN 6 (1-30 μM) suppresses the bidirectional outward and inward INCX in a concentration-dependent manner, with IC50 values of 2.3 μM and 1.9 μM, respectively. SN 6 also inhibits bidirectional current (INCX) in a [Na+]i concentration-dependent manner, with IC50 values of 3.4 μM, 2.3 μM, and 1.1 μM at 10 mM, 20 mM, and 30 mM [Na+]i, respectively[2]. SN 6 inhibits hypoxia/reoxygenation-induced LDH release with an IC50 value of 0.63 ± 0.15 μM in NCX1 transfectants[3].

References:
[1]. Iwamoto T, et al. The exchanger inhibitory peptide region-dependent inhibition of Na+/Ca2+ exchange by SN-6 [2-[4-(4-nitrobenzyloxy)benzyl]thiazolidine-4-carboxylic acid ethyl ester], a novel benzyloxyphenyl derivative. Mol Pharmacol. 2004 Jul;66(1):45-55.
[2]. Niu CF, et al. Electrophysiological effects of SN-6, a novel Na+/Ca2+ exchange inhibitor on membrane currents in guinea pig ventricular myocytes. Ann N Y Acad Sci. 2007 Mar;1099:534-9.
[3]. Kita S, et al. Inhibitory mechanism of SN-6, a novel benzyloxyphenyl Na+/Ca2+ exchange inhibitor. Ann N Y Acad Sci. 2007 Mar;1099:529-33.

Protocol

Cell experiment:

Na+i-dependent 45Ca2+ uptake into cells expressing the wild-type or mutated exchangers are assayed. In brief, confluent transfectants in 24-well dishes are loaded with Na+ by incubation at 37°C for 40 min in 0.5 mL of balanced salt solution (BSS) (10 mM HEPES/Tris, pH 7.4, 146 mM NaCl, 4 mM KCl, 2 mM MgCl2, 0.1 mM CaCl2, 10 mM glucose, and 0.1% bovine serum albumin) containing 1 mM ouabain and 10 μM monensin. 45Ca2+ uptake is then initiated by switching the medium to Na+-free BSS (replacing NaCl with equimolar choline chloride) or to normal BSS, both of which contain 0.1 mM 45CaCl2 (370 kBq/mL) and 1 mM ouabain. After a 30-s incubation, 45Ca2+ uptake is terminated by washing cells four times with an ice-cold solution containing 10 mM HEPES/Tris, pH 7.4, 120 mM choline chloride, and 10 mM LaCl3. Cells are then solubilized with 0.1 N NaOH, and aliquots are taken for determination of radioactivity and protein. When present, SN 6 and KB-R7943 are included in the medium 15 min before the start of 45Ca2+ uptake[1].

References:

[1]. Iwamoto T, et al. The exchanger inhibitory peptide region-dependent inhibition of Na+/Ca2+ exchange by SN-6 [2-[4-(4-nitrobenzyloxy)benzyl]thiazolidine-4-carboxylic acid ethyl ester], a novel benzyloxyphenyl derivative. Mol Pharmacol. 2004 Jul;66(1):45-55.
[2]. Niu CF, et al. Electrophysiological effects of SN-6, a novel Na+/Ca2+ exchange inhibitor on membrane currents in guinea pig ventricular myocytes. Ann N Y Acad Sci. 2007 Mar;1099:534-9.
[3]. Kita S, et al. Inhibitory mechanism of SN-6, a novel benzyloxyphenyl Na+/Ca2+ exchange inhibitor. Ann N Y Acad Sci. 2007 Mar;1099:529-33.

Product Documents

Purity:>99.50%Appearance:A solid

Chemical Properties

CAS No.
415697-08-4
Chemical Name
(2S,4R)-ethyl 2-(4-((4-nitrobenzyl)oxy)benzyl)thiazolidine-4-carboxylate
SMILES
O=C([C@H]1N[C@H](CC(C=C2)=CC=C2OCC(C=C3)=CC=C3[N+]([O-])=O)SC1)OCC
Molecular Formula
C20H22N2O5S
Molecular Weight
402.16
Solubility
DMSO : 62.5 mg/mL (155.29 mM; Need ultrasonic)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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