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)。


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| 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). |
| 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 |
| 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 |
| 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 |
|
| 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 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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