Lubeluzole
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.
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- CAS No.: 144665-07-6
- 화학식: C22H25F2N3O2S
- 분자량:433.51
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
5.7 μM
Compound: (S)-1a, Lubeluzole
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Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
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[PMID: 23886686] |
| A549 | IC50 |
14 μM
Compound: (S)-1a, Lubeluzole
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Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
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[PMID: 23886686] |
| CHO | IC50 |
0.26 μM
Compound: Lubeluzole
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In vitro inhibition of [14C]- guanidinium influx in Chinese hamster ovary (CHO) cells expressing rat brain sodium channel type IIA (CNaIIA-1)
In vitro inhibition of [14C]- guanidinium influx in Chinese hamster ovary (CHO) cells expressing rat brain sodium channel type IIA (CNaIIA-1)
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[PMID: 9685245] |
| Sf9 | IC50 |
40 μM
Compound: (S)-1
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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
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[PMID: 27043269] |
Lubeluzole (0.1-100 nM, 19 h) protects neurons from glutamate-induced excitotoxicity in primary mixed hippocampal cultures[1].
Lubeluzole (64-128 μg/mL) inhibits Yersinia enterocolitica DSM 4780 and Bacillus cereus DSM 4313[2].
Lubeluzole (25.6-204.8 μg/mL) exhibits synergistic antibacterial effects against Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 25922 companied with Minocycline (HY-17412A)[2].
Lubeluzole (0.001-1 μM, 30 mins) inhibits acetylcholine-induced contraction in the isolated rat proximal colon model[2].
Lubeluzole (0.01-100 μM) inhibits cardiac sodium channels (INa) in isolated guinea-pig ventricular myocytes[3].
Lubeluzole (0.001-1 μM) lengthens action potential duration at 50% and 90% of repolarization in rabbit isolated Purkinje fibres[4].
Lubeluzole (0.005-100 μM, 72 h) exhibits anti-proliferative activity in A2780/DX3, A2780, A549, MDA-MB-231, and HepG2 cells, with IC50 values ranging from 4.7 to 29.6 μM[5].
Lubeluzole (0.5-50 μM, 72 h) synergistically induces apoptosis companied with Doxorubicin (HY-15142A) in A2780/DX3 and A2780 cells[5].
Lubeluzole (6.5-30.8 μM, 4 h) increases Doxorubicin accumulation in A2780/DX3 cells[5].
Lubeluzole (6.5-30.8 μM, 72 h) downregulates MDR1 expression in A2780/DX3 cells[5].
Lubeluzole (0.05-0.5 μM, 1 h) synergistically enhances Doxorubicin-induced oxidative stress damage in A2780/DX3 cells[5].
Lubeluzole (0.005-0.5 μM, 18 h) reduces intracellular NO levels in A2780/DX3 cells[5].
Lubeluzole (7.3623.6 μM, 16 h) inhibits cell invasion in MDA-MB-231 cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lubeluzole (0.63-2.5 mg/kg, half dose via i.p. and the other half dose via i.v. over 1 h, immediately after MCAO) reduces infarct volume in MCAO rats models[1].
Lubeluzole (2.5 mg/kg, half dose via i.p. and the other half dose via i.v. over 1 h, 3 h after MCAO) reduces infarct volume in MCAO rats models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCAO rats models[1]
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Dosage:0.63, 1.25 and 2.5 mg/kg
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Administration:Half dose via i.p. and the other half dose via i.v., over 1 h, immediately after MCAO
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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.
Chemical Information
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CAS No. 144665-07-6
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분자량 433.51
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화학식 C22H25F2N3O2S
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SMILES
CN(C1CCN(CC1)C[C@H](O)COC2=CC(F)=C(C=C2)F)C3=NC4=CC=CC=C4S3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lubeluzole Related Classifications
HY-105084 Related Classifications
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