Lubeluzole dihydrochloride 

Lubeluzole dihydrochloride is the dihydrochloride salt of Lubeluzole (HY-105084). Lubeluzole is the S-isomer of benzothiazole derivative. Lubeluzole can inhibit glutamate release, glutamate-activated NO synthesis and block voltage-gated Sodium Channel and Calcium Channel. Lubeluzole exhibits anti-ischemic and neuroprotective effects. Lubeluzole also shows anti-bacterial and anti-diarrheal potential. Lubeluzole can inhibit cardiac sodium channel and prolong cardiac action potential. Lubeluzole can inhibit cancer cells proliferation and invasion and shows chemosensitizing effect. Lubeluzole can be used for the researches of cancer, infection, neurological and cardiovascular disease such as stroke, infectious diarrhea and ovarian^{[1][2][3][4][5]}.

Lubeluzole (0.1-100 nM, 19 h) 可保护原代混合海马培养物中的神经元免受谷氨酸诱导的兴奋性毒性损伤^[1]。
Lubeluzole (64-128 μg/mL) 能抑制小肠结肠炎耶尔森菌 (Yersinia enterocolitica) DSM 4780 和蜡样芽孢杆菌 (Bacillus cereus) DSM 4313^[2]。
Lubeluzole (25.6-204.8 μg/mL) 与 Minocycline (HY-17412A) 联合使用时，对粪肠球菌 (Enterococcus faecalis) ATCC 29212、金黄色葡萄球菌 (Staphylococcus aureus) ATCC 29213、铜绿假单胞菌 (Pseudomonas aeruginosa) ATCC 27853 和大肠杆菌 (Escherichia coli) ATCC 25922 表现出协同抗菌作用^[2]。
Lubeluzole (0.001-1 μM, 30 mins) 在离体大鼠近端结肠模型中可抑制乙酰胆碱诱导的收缩^[2]。
Lubeluzole (0.01-100 μM) 可抑制离体豚鼠心室肌细胞中的心脏钠通道 (I_Na)^[3]。
Lubeluzole (0.001-1 μM) 可延长兔离体浦肯野纤维在复极化 50% 和 90% 时的动作电位时程^[4]。
Lubeluzole (0.005-100 μM, 72 h) 在 A2780/DX3、A2780、A549、MDA-MB-231 和 HepG2 细胞中表现出抗增殖活性，其 IC₅₀ 值范围为 4.7 至 29.6 μM^[5]。
Lubeluzole (0.5-50 μM, 72 h) 与 Doxorubicin (HY-15142A) 联合使用时，可协同诱导 A2780/DX3 和 A2780 细胞凋亡^[5]。
Lubeluzole (6.5-30.8 μM, 4 h) 可增加 A2780/DX3 细胞中 Doxorubicin 的积累^[5]。
Lubeluzole (6.5-30.8 μM, 72 h) 可下调 A2780/DX3 细胞中 MDR1 的表达^[5]。
Lubeluzole (0.05-0.5 μM, 1 h) 可协同增强 Doxorubicin 诱导的 A2780/DX3 细胞氧化应激损伤^[5]。
Lubeluzole (0.005-0.5 μM, 18 h) 可降低 A2780/DX3 细胞内的 NO 水平^[5]。
Lubeluzole (7.3623.6 μM, 16 h) 可抑制 MDA-MB-231 细胞的侵袭^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lubeluzole (0.31-2.5 mg/kg，腹腔注射，MCAO 后立即给药) 可显著减小永久性大脑中动脉闭塞 (MCAO) 小鼠的脑表面梗死面积^[1]。
Lubeluzole (0.63-2.5 mg/kg，一半剂量腹腔注射，另一半剂量在 1 小时内静脉注射，MCAO 后立即给药) 可减小 MCAO 大鼠的梗死体积^[1]。
Lubeluzole (2.5 mg/kg，一半剂量腹腔注射，另一半剂量在 1 小时内静脉注射，MCAO 后 3 小时给药) 可减小 MCAO 大鼠的梗死体积^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

506.44

C₂₂H₂₇Cl₂F₂N₃O₂S

144665-09-8

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

• [1]. Culmsee C, et al. Lubeluzole protects hippocampal neurons from excitotoxicity in vitro and reduces brain damage caused by ischemia. Eur J Pharmacol. 1998 Jan 26;342(2-3):193-201.  [Content Brief]

  [2]. Cavalluzzi MM, et al. Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies. Pharmacol Rep. 2021 Feb;73(1):172-184.  [Content Brief]

  [3]. Le Grand B, et al. Study of the interaction of lubeluzole with cardiac sodium channels. J Cardiovasc Pharmacol. 2003 Nov;42(5):581-7.  [Content Brief]

  [4]. Le Grand B, et al. Lubeluzole-induced prolongation of cardiac action potential in rabbit Purkinje fibres. Fundam Clin Pharmacol. 2000 Mar-Apr;14(2):159-62.  [Content Brief]

  [5]. Viale M, et al. Lubeluzole Repositioning as Chemosensitizing Agent on Multidrug-Resistant Human Ovarian A2780/DX3 Cancer Cells. Molecules. 2022 Nov 15;27(22):7870.  [Content Brief]