Lomerizine dihydrochloride
Based on 1 publication(s) in Google Scholar
Lomerizine dihydrochloride is an antagonist of L- and T-type voltagegated calcium channels.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 101477-54-7
- Formula: C27H32Cl2F2N2O3
- Molecular Weight:541.46
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Storage:
4°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
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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HY-Y1888
Corn oil
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HY-B0293
Butoconazole nitrate
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HY-B0768AR
Lomerizine dihydrochloride (Standard)
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HY-B0280
Ranolazine
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HY-B0424
Nitrendipine
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HY-B0532A
Trifluoperazine dihydrochloride
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HY-17401
Ranolazine dihydrochloride
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HY-B0532AR
Trifluoperazine dihydrochloride (Standard)
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HY-17436
Clevidipine
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HY-B0424R
Nitrendipine (Standard)
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HY-17436R
Clevidipine (Standard)
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HY-B0280R
Ranolazine (Standard)
Publications Citing Use of MedChemExpress (MCE) Lomerizine dihydrochloride
MoreAll Calcium Channel Isoforms
More
Biological Activity
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T-type calcium channel |
L-type calcium channel |
Lomerizine is an antagonist of L- and T-type voltagegated calcium channels and transient receptor potential channel 5 transient receptor potential channels. Lomerizine is a dual L/T-type channel blocker used for prophylaxis of migraine. To demonstrate the effectiveness of Lomerizine in limiting intracellular [Ca2+], its ability to inhibit glutamate-induced death of motor neurons and the associated rise in cytosolic [Ca2+] is evaluated. Lomerizine inhibits the low- and high-voltage activated Ca2+ currents in dissociated rat brain neurons at a threshold concentration of 0.01 μM and IC50 of 1.9 μM and H2O2-induced Ca2+ influx in hippocampal neurons is inhibited by 1 μM Lomerizine. Pre-treatment with 1 μM Lomerizine significantly reduces acute death of motor neurons in spinal cord-DRG cultures exposed to 50 μM glutamate, a concentration that kills approximately 40% of motor neurons in the culture by 6 h, and inhibits the rise in cytosolic [Ca2+] that occurs with glutamate treatment. 0.5 μM Lomerizine is sufficient to significantly prevent the mitochondrial fragmentation of mitochondria induced by SOD1G93A[1]. Lomerizine increases the cytotoxicity of Adriamycin (ADM) and the apoptosis induced by ADM or Vincristine (VCR) in K562/ADM cells. At the concentration of 3, 10 and 30μM, Lomerizine reduces the IC50 value of ADM from 79.03 μM to 28.14, 8.16 and 3.16 μM, respectively. Lomerizine increases the intracellular accumulation of ADM and inhibits the efflux of Rh123 in K562/ ADM cells. No change in P-gp expression is observed after the treatment of Lomerizine for 72 h. Lomerizine has strong reversal effect on MDR in K562/ADM cells by inhibiting P-gp function[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 101477-54-7
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Appearance Solid
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Molecular Weight 541.46
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Formula C27H32Cl2F2N2O3
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Color White to off-white
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SMILES
COC1=CC=C(CN2CCN(C(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2)C(OC)=C1OC.[H]Cl.[H]Cl
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Synonyms
KB-2796
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Med Rep
Identification of metabolites associated with capecitabine‑induced hand‑foot syndrome using untargeted metabolomics in patients with cancer. [Abstract]2025 Jul;32(1):203. PMID: 40377002
Solvent & Solubility
DMSO : 125 mg/mL (230.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
MTT assay is used to determine the influence of Lomerizine on the cytotoxicity of Adriamycin (ADM). The effect of Lomerizine (3, 10 and 30 μM) on the apoptosis induced by ADM and Vincristine (VCR) in K562/ADM cells is detected using flow cytometry. Intracellular accumulation of ADM is measured by fluorescence spectrophotometry. Flow cytometry is used to investigate the efflux of Rhodamine 123 (Rh123) and the expression of P-glycoprotein (P-gp) in K562/ADM cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
The p50-deficient mice and wild-type mice aged 2 months are daily pre-treated intraperitoneally with Memantine (10 mg/kg), MK-801 (0.5 mg/kg), Lomerizine (1 mg/kg), or Tacrolimus (2, 0.5 and 0.2 mg/kg) for one week before the NMDA injection. These mice are given an intravitreous injection of 5 nM NMDA, which is a relatively low concentration for causing neurotoxicity[3].
Rats[4]
Male Wistar rats weighing 250 to 350 g are housed in an air-conditioned room at 25±0°C with 55±5% humidity and given food and water ad libitum. Lomerizine is injected i.v. in a volume of 1 mL/kg body weight. Effects of Lomerizine (0.3 mg/kg, i.v., or 1 mg/kg, i.v.) are measured on cerebral cortical blood flow measured by laser Doppler flowmetry (CBFLDF) in anaesthetized rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
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Handling Instructions (2659 KB)
References
[1]. Tran LT, et al. The voltage-gated calcium channel blocker Lomerizine is neuroprotective in motor neurons expressing mutant SOD1, but not TDP-43. J Neurochem. 2014 Aug;130(3):455-66. [Content Brief]
[2]. Zhu HJ, et al. [Reversal of multidrug resistance by Lomerizine in K562/ADM cells]. Yao Xue Xue Bao. 2004 May;39(5):333-7. [Content Brief]
[3]. Nakamura-Yanagidaira T, et al. Development of spontaneous neuropathy in NF-κBp50-deficient mice by calcineurin-signal involving impaired NF-κB activation. Mol Vis. 2011;17:2157-70. [Content Brief]
[4]. Shimazawa M, et al. Effects of Ca2+ channel blockers on cortical hypoperfusion and expression of c-Fos-like immunoreactivity after cortical spreading depression in rats. Br J Pharmacol. 1995 Aug;115(8):1359-68. [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 |
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| DMSO | 1 mM | 1.8469 mL | 9.2343 mL | 18.4686 mL | 46.1715 mL |
| 5 mM | 0.3694 mL | 1.8469 mL | 3.6937 mL | 9.2343 mL | |
| 10 mM | 0.1847 mL | 0.9234 mL | 1.8469 mL | 4.6171 mL | |
| 15 mM | 0.1231 mL | 0.6156 mL | 1.2312 mL | 3.0781 mL | |
| 20 mM | 0.0923 mL | 0.4617 mL | 0.9234 mL | 2.3086 mL | |
| 25 mM | 0.0739 mL | 0.3694 mL | 0.7387 mL | 1.8469 mL | |
| 30 mM | 0.0616 mL | 0.3078 mL | 0.6156 mL | 1.5390 mL | |
| 40 mM | 0.0462 mL | 0.2309 mL | 0.4617 mL | 1.1543 mL | |
| 50 mM | 0.0369 mL | 0.1847 mL | 0.3694 mL | 0.9234 mL | |
| 60 mM | 0.0308 mL | 0.1539 mL | 0.3078 mL | 0.7695 mL | |
| 80 mM | 0.0231 mL | 0.1154 mL | 0.2309 mL | 0.5771 mL | |
| 100 mM | 0.0185 mL | 0.0923 mL | 0.1847 mL | 0.4617 mL |
Lomerizine dihydrochloride Related Classifications
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