Lubeluzole
CAS No. : 144665-07-6
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| Cat. No. : | HY-105084 |
| M.Wt: | 433.51 |
| Formula: | C22H25F2N3O2S |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
In Vitro: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].
In Vivo:Lubeluzole (0.31-2.5 mg/kg, i.p., immediately after MCAO) significantly reduces the infarct area on the brain surface in permanent middle cerebral artery occlusion (MCAO) mice models[1].
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].
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