SN-6 |
Katalog-Nr.GC15195
One-Click Copy Product Info
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SN-6 ist ein selektiver Na+/Ca2+-Austauscher (NCX)-Inhibitor und hemmt die 45Ca2+-Aufnahme durch NCX1, NCX2 und NCX3 mit IC50-Werten von 2,9, 16 bzw. 8,6 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 415697-08-4
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 415697-08-4 | SDF | |
| Chemical Name | (2S,4R)-ethyl 2-(4-((4-nitrobenzyl)oxy)benzyl)thiazolidine-4-carboxylate | ||
| Canonical SMILES | O=C([C@H]1N[C@H](CC(C=C2)=CC=C2OCC(C=C3)=CC=C3[N+]([O-])=O)SC1)OCC | ||
| Formula | C20H22N2O5S | M.Wt | 402.16 |
| Löslichkeit | DMSO : 62.5 mg/mL (155.29 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4866 mL | 12.4329 mL | 24.8657 mL |
| 5 mM | 497.3 μL | 2.4866 mL | 4.9731 mL |
| 10 mM | 248.7 μL | 1.2433 mL | 2.4866 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)