Lubeluzole dihydrochloride
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Lubeluzole dihydrochloride is the dihydrochloride salt of Lubeluzole (HY-105084). Lubeluzole dihydrochloride is the S-isomer of benzothiazole derivative. Lubeluzole dihydrochloride can inhibit glutamate release, glutamate-activated NO synthesis and block voltage-gated Sodium Channel and Calcium Channel. Lubeluzole dihydrochloride exhibits anti-ischemic and neuroprotective effects. Lubeluzole dihydrochloride also shows anti-bacterial and anti-diarrheal potential. Lubeluzole dihydrochloride can inhibit cardiac sodium channel and prolong cardiac action potential. Lubeluzole dihydrochloride can inhibit cancer cells proliferation and invasion and shows chemosensitizing effect. Lubeluzole dihydrochloride can be used for the researches of cancer, infection, neurological and cardiovascular disease such as stroke, infectious diarrhea and ovarian.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 144665-09-8
- Formula: C22H27Cl2F2N3O2S
- Molecular Weight:506.44
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Lubeluzole (0.1-100 nM, 19 h) dihydrochloride protects neurons from glutamate-induced excitotoxicity in primary mixed hippocampal cultures[1].
Lubeluzole (64-128 μg/mL) dihydrochloride inhibits Yersinia enterocolitica DSM 4780 and Bacillus cereus DSM 4313[2].
Lubeluzole (25.6-204.8 μg/mL) dihydrochloride 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 (HY17412A)[2].
Lubeluzole (0.001-1 μM, 30 mins) dihydrochloride inhibits acetylcholine-induced contraction in the isolated rat proximal colon model[2].
Lubeluzole (0.01-100 μM) dihydrochloride inhibits cardiac sodium channels (INa) in isolated guinea-pig ventricular myocytes[3].
Lubeluzole (0.001-1 μM) dihydrochloride lengthens action potential duration at 50% and 90% of repolarization in rabbit isolated Purkinje fibres[4].
Lubeluzole (0.005-100 μM, 72 h) dihydrochloride 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) dihydrochloride synergistically induces apoptosis companied with Doxorubicin (HY-15142A) in A2780/DX3 and A2780 cells[5].
Lubeluzole (6.5-30.8 μM, 4 h) dihydrochloride increases Doxorubicin accumulation in A2780/DX3 cells[5].
Lubeluzole (6.5-30.8 μM, 72 h) dihydrochloride downregulates MDR1 expression in A2780/DX3 cells[5].
Lubeluzole (0.05-0.5 μM, 1 h) dihydrochloride synergistically enhances Doxorubicin-induced oxidative stress damage in A2780/DX3 cells[5].
Lubeluzole (0.005-0.5 μM, 18 h) dihydrochloride reduces intracellular NO levels in A2780/DX3 cells[5].
Lubeluzole (7.3623.6 μM, 16 h) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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. 144665-09-8
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Appearance Solid
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Molecular Weight 506.44
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Formula C22H27Cl2F2N3O2S
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Color White to off-white
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SMILES
CN(C1CCN(CC1)C[C@H](O)COC2=CC(F)=C(C=C2)F)C3=NC4=CC=CC=C4S3.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 2 mg/mL (3.95 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.9746 mL | 9.8728 mL | 19.7457 mL | 49.3642 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Lubeluzole dihydrochloride Related Classifications
HY-105084A Related Classifications
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