SN-6
目录号 : GC15195
SN-6 是一种选择性 Na+/Ca2+ 交换剂 (NCX) 抑制剂，可抑制 NCX1、NCX2 和 NCX3 对 45Ca2+ 的摄取，IC50 分别为 2.9、16 和 8.6 μM。
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 | |
| 化学名 | (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 | ||
| 分子式 | C20H22N2O5S | 分子量 | 402.16 |
| 溶解度 | DMSO : 62.5 mg/mL (155.29 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4866 mL | 12.4329 mL | 24.8657 mL |
| 5 mM | 0.4973 mL | 2.4866 mL | 4.9731 mL |
| 10 mM | 0.2487 mL | 1.2433 mL | 2.4866 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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