Clemastine fumarate
Based on 15 publication(s) in Google Scholar
Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
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- Pureza : 99.96%
- No. CAS: 14976-57-9
- Fòrmula: C25H30ClNO5
- Peso molecular:459.96
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Clemastine fumarate
More- Redox Biol. 2025 Sep 20:87:103875. [Abstract]
- Acta Pharmacol Sin. 2026 Jun 23. [Abstract]
- Cell Prolif. 2021 Jan;54(1):e12953. [Abstract]
- Br J Pharmacol. 2025 Jun;182(12):2730-2753. [Abstract]
- J Ethnopharmacol. 2027 Jan 10:372:122159.
- Neurosci Bull. 2025 Jul 17. [Abstract]
- Exp Neurol. 2025 Mar:385:115086. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2024 Feb 8:129:110901. [Abstract]
- Microbiol Spectr. 2022 Apr 27;10(2):e0054121. [Abstract]
- Viruses. 2021 Jun 28;13(7):1255. [Abstract]
- Biochem Biophys Res Commun. 2020 Feb 19;522(4):862-868. [Abstract]
- Biomed Pharmacother. 2026 Sep:202:119803.
- Res Sq. 2026 Jun 25.
- Res Sq. 2026 Mar 23.
- Methods Mol Biol. 2023:2683:103-111. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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WB
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RT-PCR
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Microbiological Assay
Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
H1 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>50 μM
Compound: 92125238
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HARVARD: Cytotoxicity in HepG2 cell line
HARVARD: Cytotoxicity in HepG2 cell line
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[PMID: 22586124] |
| HepG2 | IC50 |
0.951 μM
Compound: 92125238
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HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
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[PMID: 22586124] |
| Huh-7 | CC50 |
>100 μM
Compound: Clemastine fumarate
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Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by luminometric method
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by luminometric method
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[PMID: 34394844] |
In Vitro
Clemastine (fumarate) (HS-592 (fumarate)) inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively[1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26 hours after administration, and by the biphasic decline in plasma concentration. The terminal elimination half-life (t1/2) of clemastine was 21.3 +/- 11.6 hours. Steady-state concentrations of clemastine were consistent with linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or by race[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 14976-57-9
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Appearance Solid
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Peso molecular 459.96
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Fòrmula C25H30ClNO5
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Color White to off-white
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SMILES
CN1[C@@H](CCO[C@](C2=CC=CC=C2)(C3=CC=C(Cl)C=C3)C)CCC1.O=C(O)/C=C/C(O)=O
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Synonyms
HS-592 fumarate; Meclastine fumarate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (15)
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Journal Impact Factor
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Most Recent
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Redox Biol
Sigma-1 receptor counteracts non-cell-autonomous poly-PR-induced astrocytic oxidative stress in C9orf72 ALS. [Abstract]2025 Sep 20:87:103875. PMID: 40992079
Clemastine fumarate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Sep 20:87:103875. [Abstract]
Immunoprecipitation analysis of BiP-Sigma-1R interaction following Clemastine fumarate (0-7.5 μM) treatment. Sigma-1R agonist activity leads to dissociation from BiP, indicative of functional activation.
Clemastine fumarate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Sep 20:87:103875. [Abstract]
Quantification of BiP associated with Sigma-1R showed a significant reduction at 2.5 μM Clemastine fumarate.
Clemastine fumarate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Sep 20:87:103875. [Abstract]
Western blot analysis of NOX4 protein levels in astrocytes treated with exogenous poly-PR20, with or without 2.5 μM Clemastine fumarate.
Clemastine fumarate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Sep 20:87:103875. [Abstract]
RT-qPCR analysis showed decreased NOX4 mRNA expression in Clemastine fumarate-treated astrocytes under poly-PR20 conditions.
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Acta Pharmacol Sin
Clemastine alleviates cognitive dysfunction after SAH by targeting neuronal CNTN1 to regulate the ADA-adenosine pathway. [Abstract]2026 Jun 23. PMID: 42337055 -
Cell Prolif
Direct inhibitory effect on viral entry of influenza A and SARS-CoV-2 viruses by azithromycin. [Abstract]2021 Jan;54(1):e12953. PMID: 33211371 -
Br J Pharmacol
Clemastine attenuates subarachnoid haemorrhage pathology in a mouse model via Nrf2/SQSTM1-mediated autophagy. [Abstract]2025 Jun;182(12):2730-2753. PMID: 40052261 -
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Neurosci Bull
Hippocampal Oligodendrocytes Regulate Mossy Fiber Development Involved in Epileptic Responses. [Abstract]2025 Jul 17. PMID: 40673958 -
Exp Neurol
Inhibition of histamine receptor 3 alleviates sevoflurane-induced hypomyelination and neurobehavioral deficits. [Abstract]2025 Mar:385:115086. PMID: 39637962 -
Prog Neuropsychopharmacol Biol Psychiatry
Demyelination in the medial prefrontal cortex by withdrawal from chronic nicotine causes impaired cognitive memory. [Abstract]2024 Feb 8:129:110901. PMID: 38036034 -
Microbiol Spectr
Clemastine Inhibits the Biofilm and Hemolytic of Staphylococcus aureus through the GdpP Protein. [Abstract]2022 Apr 27;10(2):e0054121. PMID: 35234502
Clemastine fumarate purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Apr 27;10(2):e0054121. [Abstract]
The Clemastine fumarate with a series of inhibitory concentrations inhibited the biofilm formation of S. aureus by the crystal violet staining method. YuSA80, YUSA139, YuSA145, CHS350, CHS712, and CHS101 strains were incubated with Clemastine fumarate 24 h at a series of concentrations of 0, 6.25, 12.5, 25, and 50 μM. The biofilm was then measured by crystal violet staining. The biofilm formation of six S. aureus strains was inhibited by clemastine at 50 μM.
Clemastine fumarate purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Apr 27;10(2):e0054121. [Abstract]
The Clemastine fumarate inhibited the biofilm formation of S. aureus observed by CLSM. Twenty-four-hour-old biofilms of MSSA SA113 and MRSA YUSA145 were grown on cover glass in a cell culture dish and observed by CLSM. Three-dimensional (3D) structural images were reconstructed. Viable and dead cells were stained green (SYTO9) and red (PI), respectively.
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Viruses
Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]2021 Jun 28;13(7):1255. PMID: 34203149 -
Biochem Biophys Res Commun
Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]2020 Feb 19;522(4):862-868. PMID: 31806372 -
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Methods Mol Biol
Characterizing the Neuron-Glial Interactions by the Co-cultures of Human iPSC-Derived Oligodendroglia and Neurons. [Abstract]2023:2683:103-111. PMID: 37300770
Solvente y solubilidad
In Vitro:
DMSO : 10.29 mg/mL (22.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.67 mg/mL (1.46 mM; Need ultrasonic)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* 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)
In Vivo:
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: ≥ 1.43 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 1.43 mg/mL (3.11 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
In Vivo Dissolution Calculator
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, 1 year; -20°C, 6 months (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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zou Y, et al. Clemastine attenuates subarachnoid haemorrhage pathology in a mouse model via Nrf2/SQSTM1-mediated autophagy. Br J Pharmacol. 2025;182(12):2730-2753. [Content Brief]
[2]. Kocot J, et al. Clemastine fumarate accelerates accumulation of disability in progressive multiple sclerosis by enhancing pyroptosis. J Clin Invest. 2025;135(10):e183941. Published 2025 May 15. [Content Brief]
[3]. Yamazaki R, et al. The potential of repurposing clemastine to promote remyelination. Front Cell Neurosci. 2025;19:1582902. Published 2025 May 7. [Content Brief]
[4]. Myatich A, et al. Clemastine in remyelination and protection of neurons and skeletal muscle after spinal cord injury. Neural Regen Res. 2023;18(5):940-946. [Content Brief]
[5].
Wang X, et al. Clemastine protects against sepsis-induced myocardial injury in vivo and in vitro. Bioengineered. 2022 Mar;13(3):7134-7146.
[Content Brief]
[6]. Liu K, et al. Remyelination-oriented clemastine treatment attenuates neuropathies of optic nerve and retina in glaucoma. Glia. 2024;72(9):1555-1571. [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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1741 mL | 10.8705 mL | 21.7410 mL | 54.3526 mL |
| DMSO | 5 mM | 0.4348 mL | 2.1741 mL | 4.3482 mL | 10.8705 mL |
| 10 mM | 0.2174 mL | 1.0871 mL | 2.1741 mL | 5.4353 mL | |
| 15 mM | 0.1449 mL | 0.7247 mL | 1.4494 mL | 3.6235 mL | |
| 20 mM | 0.1087 mL | 0.5435 mL | 1.0871 mL | 2.7176 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.
Clemastine fumarate Related Classifications
HY-B0298A Related Classifications
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