Name | ethyl 2-[[4-[(4-nitrophenyl)methoxy]phenyl]methyl]-1,3-thiazolidine-4-carboxylate |
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Synonyms |
hms3268p11
sn-6 SN 6 |
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. |
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Related Catalog | |
Target |
IC50:2.9 μM (NCX1), 16 μM (NCX2), 8.6 μM (NCX3)[1] |
In Vitro | 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]. |
Cell Assay | 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 |
Density | 1.285g/cm3 |
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Boiling Point | 581.2ºC at 760mmHg |
Molecular Formula | C20H22N2O5S |
Molecular Weight | 402.46400 |
Flash Point | 305.3ºC |
Exact Mass | 402.12500 |
PSA | 118.68000 |
LogP | 4.16250 |
Index of Refraction | 1.605 |
Storage condition | -20℃ |