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S0859 {[allProObj[0].p_purity_real_show]}

货号:A676229

S0859 是一种选择性、高亲和力的 Na+/HCO3- 协同转运体 (NBC) 抑制剂,可逆地抑制 NBC 介导的细胞内 pH 恢复 (Ki=1.7 μM,30 μM 时完全抑制)。

S0859 化学结构 CAS号:1019331-10-2
S0859 化学结构
CAS号:1019331-10-2
S0859 3D分子结构
CAS号:1019331-10-2
S0859 化学结构 CAS号:1019331-10-2
S0859 3D分子结构 CAS号:1019331-10-2
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S0859 纯度/质量文件 产品仅供科研

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S0859 生物活性

描述 S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH (i) recovery (K (i)=1.7 mM, full inhibition at approximately 30 mM).

S0859 细胞实验

Cell Line
Concentration Treated Time Description References
A549 cells 20 µM 24 hours To evaluate the effect of S0859 on cell migration, results showed that S0859 partially inhibited cell motility. Pharmaceutics. 2020 Aug 27;12(9):816
Mouse hippocampal neurons 50 µM 30 minutes To investigate the effect of S0859 on GABA A receptor-mediated postsynaptic currents. Results showed that S0859 completely inhibited postsynaptic GABA AR and, thus, could not be used as a tool to investigate the role of NBCs in GABA-dependent neuronal networks. Front Cell Neurosci. 2023 Oct 10;17:1253424
HEK-293 cells 50 µM 30 minutes To investigate the effect of NBC inhibitor S0859 on KCC2 activity. Results showed that S0859 prevented staurosporine- and 4-aminopyridine(4AP)-induced KCC2 activation. Front Cell Neurosci. 2023 Oct 10;17:1253424
Mouse renal afferent arterioles 50 µM 30 minutes S0859, an inhibitor of the NBC family, blocked the NaHCO3-induced increase in pH i and vasodilation Hypertension. 2019 Nov;74(5):1104-1112
LNCaP cells 50 µM 4 days To assess the role of NBCe1 in LNCaP cell proliferation and viability, results showed that S0859 treatment decreased the number of viable cells Oncol Rep. 2021 Jul;46(1):129
Ciliated human nasal epithelial cells (c-hNECs) 30 µM 5 minutes S0859 decreased the CBF ratio from 1.00 to 0.79, indicating that the NBC inhibitor reduced HCO3- influx, thereby lowering pH i and CBF. Int J Mol Sci. 2024 Aug 21;25(16):9069
PC3 cells 100 µM 6 days To assess the role of NBCe1 in PC3 cell proliferation and viability, results showed that S0859 treatment decreased the number of viable cells Oncol Rep. 2021 Jul;46(1):129
Human keratinocytes (HaCaT) 100 µM 6 hours To evaluate the inhibitory effect of S0859 on SLS-induced cytotoxicity in keratinocytes. Results showed that S0859 significantly inhibited SLS-dependent cell death. Front Cell Infect Microbiol. 2022 Nov 1;12:1002230
RA-FLSs (rheumatoid arthritis fibroblast-like synoviocytes) 20 µM 6 hours To evaluate the inhibitory effect of S0859 on RA-FLSs migration. Results showed that S0859 significantly reduced TNF-α or RA synovial fluid-stimulated RA-FLSs migration. Exp Mol Med. 2022 Apr;54(4):503-517
MCF-7 cells 50 µM 7 days To evaluate the effect of S0859 on MCF-7 spheroid growth, results showed that S0859 combined with MCT1 inhibitor AR-C155858 further reduced spheroid diameter Mol Cancer. 2016 Jun 6;15(1):45

S0859 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Necrotizing skin infection model Subcutaneous injection 200 µM Initial injection followed by additional doses at 4 and 8 hours post-infection, lasting 24 hours To evaluate the effect of S0859 on SLS-dependent skin lesions. Results showed that S0859 treatment did not significantly affect SLS-mediated skin lesion size. Front Cell Infect Microbiol. 2022 Nov 1;12:1002230
DBA/1 mice Collagen-induced arthritis (CIA) model Tail vein injection 800 ng/g Two injections, two weeks apart To evaluate the inhibitory effect of S0859 on joint swelling and destruction in the CIA mouse model. Results showed that S0859 reduced joint swelling and destruction without blood, hepatic, or renal toxicity. Exp Mol Med. 2022 Apr;54(4):503-517

S0859 参考文献

[1]Larsen AM, Krogsgaard-Larsen N, et al. Gram-scale solution-phase synthesis of selective sodium bicarbonate co-transport inhibitor S0859: in vitro efficacy studies in breast cancer cells. ChemMedChem. 2012 Oct;7(10):1808-14.

[2]Ch'en FF, Villafuerte FC, et al. S0859, an N-cyanosulphonamide inhibitor of sodium-bicarbonate cotransport in the heart. Br J Pharmacol. 2008;153(5):972-82

S0859 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.43mL

1.89mL

0.94mL

18.87mL

3.77mL

1.89mL

S0859 技术信息

CAS号1019331-10-2
分子式C29H24ClN3O3S
分子量 530.04
SMILES Code O=C(N(CC1=CC=C(C2=CC=CC=C2S(=O)(NC#N)=O)C=C1)CC3=CC=C(C)C=C3)C4=CC=CC=C4Cl
MDL No. MFCD23136018
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 105 mg/mL(198.1 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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方案 三
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