2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Sodium Channel Calcium Channel
  4. Lubeluzole

Lubeluzole 是苯并噻唑衍生物的 S-异构体。Lubeluzole 能够抑制谷氨酸的释放、谷氨酸激活的 NO 合成，并阻断电压门控的钠通道 (Sodium Channel) 和钙通道 (Calcium Channel)。Lubeluzole 具有抗缺血和神经保护作用。Lubeluzole 还显示出抗菌和抗腹泻的潜力。Lubeluzole 可以抑制心肌钠通道，延长心肌动作电位。Lubeluzole 能够抑制癌细胞的增殖和侵袭，并表现出化学增敏作用。Lubeluzole 可用于癌症、感染、神经系统和心血管疾病的研究，如中风、感染性腹泻和卵巢癌。

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Lubeluzole

Lubeluzole Chemical Structure

CAS No. : 144665-07-6

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规格 价格 是否有货 数量
5 mg ￥3197
3 - 4 周
10 mg   询价  
50 mg   询价  

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
5.7 μM
Compound: (S)-1a, Lubeluzole
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
[PMID: 23886686]
A549 IC50
14 μM
Compound: (S)-1a, Lubeluzole
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 23886686]
Sf9 IC50
40 μM
Compound: (S)-1
Inhibition of full-length recombinant human CamKII expressed in insect Sf9 cells incubated for 30 mins in presence of 5 uM CaM/[gamma32P]ATP by scintillation counting analysis
Inhibition of full-length recombinant human CamKII expressed in insect Sf9 cells incubated for 30 mins in presence of 5 uM CaM/[gamma32P]ATP by scintillation counting analysis
[PMID: 27043269]
体外研究
(In Vitro)

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 (INa)[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 相关抗体:
体内研究
(In Vivo)

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.

Animal Model: MCAO rats models[1]
Dosage: 0.63, 1.25 and 2.5 mg/kg
Administration: Half dose via i.p. and the other half dose via i.v., over 1 h, immediately after MCAO
Result: Decreased the infarct volume to approximately 70%.
Did not affect physiological parameters, such as mean arterial blood pressure, blood glucose, arterial pH, pCO2 and pO2.
分子量

433.51

Formula

C22H25F2N3O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Lubeluzole 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lubeluzole144665-07-6Sodium ChannelCalcium ChannelNa channelsNa+ channelsCa2+ channelsCa channelsBenzothiazole derivativeGlutamateNO synthesisA2780/DX3chemosensitizingStrokeInfectious diarrheaOvarianNeuroprotectantInhibitorinhibitorinhibit

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