Referencia número: HY-B0298

Clemastine

(Synonyms: HS-592; Meclastine)

12 Cited Publications

Revisión del cliente

Based on 12 publication(s) in Google Scholar

Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine 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: 99.26%
No. CAS: 15686-51-8
Fòrmula: C₂₁H₂₆ClNO
Peso molecular:343.89

Almacenamiento:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Clemastine Chemical Structure

No. CAS: 15686-51-8

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (12)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

H₁ Receptor

Ver todos los productos específicos de isoformas Histamine Receptor :

Ver todos los productos específicos de isoformas mAChR :

Ver todos los productos específicos de isoformas mTOR :

Ver todos los productos específicos de isoformas IKK :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	4.9 μM Compound: clemastine	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
HeLa	IC₅₀	1.1 μM Compound: Clemastine	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]

In Vitro

Clemastine (10 μM; 12 h) promotes Nrf2 nuclear translocation, activates the Nrf2/SQSTM1 pathway, and increases autophagy-related gene transcription in Hb-treated HT-22 cells^[1].
Clemastine (10-50 μM; 1 h for DARTS assay) directly binds to the M4 receptor, and M4 receptor signalling mediates clemastine-induced activation of the Nrf2/SQSTM1/TBK1 autophagy pathway in HT-22 cells^[1].
Clemastine (10 μg/mL; 3-18 h, 90 min) potentiates ATP-induced inflammasome activation and GSDMD-dependent pyroptotic cell death in LPS-primed THP-1 cells^[2].
Clemastine (10 μg/mL; 3-18 h) potentiates ATP-induced inflammasome activation and pyroptotic cell death in LPS-primed primary human monocyte-derived macrophages via a P2RX7-dependent mechanism^[2].
Clemastine (10 μg/mL; 18 h) induces lytic cell death in LPS-primed human iPSC-derived oligodendrocytes when combined with 2 mM ATP^[2].
Clemastine promotes oligodendrocyte precursor cell differentiation into mature myelinating oligodendrocytes via CHRM1 blockade and ERK pathway activation^[3].
Clemastine induces an NMDA receptor-rich state in oligodendrocyte precursor cells by modifying their membrane properties^[3].
Clemastine (1.25 μg/mL) reduces cellular apoptosis, improves mitochondrial structural damage, and promotes autophagy in LPS-stimulated H9c2 cardiomyocytes^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Clemastine (1 mg/kg; i.p.; single administration) improves short-term neurological function, alleviates oxidative stress and neuronal death, and activates Nrf2/SQSTM1-mediated autophagy in mice with subarachnoid hemorrhage (SAH). These effects depend on the Nrf2 and mTOR signaling pathways^[1].
Clemastine (10 mg/kg; p.o.; once daily; for 28 consecutive days) reverses long-term cognitive impairment and attenuates hippocampal neuronal damage in a mouse model of subarachnoid hemorrhage (SAH)^[1].
Clemastine enhances remyelination and reverses behavioral changes in cuprizone-induced mouse models of multiple sclerosis^[2].
Clemastine accelerates remyelination, prevents axonal loss, and improves functional recovery in a mouse model of inflammatory demyelination-related multiple sclerosis^[2].
Clemastine enhances myelination in the prefrontal cortex and reverses behavioral alterations in socially isolated mice^[2].
Clemastine enhances myelination, delays axonal loss, and promotes functional recovery in mouse models of spinal cord injury^[2].
Clemastine preserves myelin integrity, reduces axonal loss, promotes oligodendrocyte differentiation, and improves motor function recovery in a rat model of spinal cord contusion injury^[4].
Clemastine promotes the differentiation of oligodendrocyte precursor cells and remyelination in a rat model of Pelizaeus-Merzbacher disease without immunosuppressive effects^[4].
Clemastine promotes remyelination in a lysophosphatidylcholine-induced demyelination mouse model^[4].
Clemastine (10-50 mg/kg; i.p.; single administration) increases the 7-day survival rate and reduces serum cTnI levels in CLP-induced septic rats; in addition, 30 mg/kg Clemastine improves cardiac function, alleviates cardiomyocyte apoptosis and mitochondrial damage, and promotes autophagy, with its anti-apoptotic effect dependent on autophagy activation^[5].
Clemastine (10 mg/kg; p.o.; once daily for 21 consecutive days) promotes oligodendrocyte precursor cell differentiation and remyelination, thereby improving the structural recovery and functional outcomes of the optic nerve and retina in a mouse model of glaucoma^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (male, 8 weeks old, subarachnoid haemorrhage model via stereotactic injection of autologous blood)^[1]
Dosage:

1 mg/kg
Administration:

i.p.; single dose
Result:

Improved modified Garcia scale scores relative to SAH + vehicle controls.
Reduced beam balance test hind limb slippage frequency relative to SAH + vehicle controls.
Reduced number of DHE-positive superoxide-producing neurons relative to SAH + vehicle controls.
Reduced number of FJC-positive degenerating neurons relative to SAH + vehicle controls.
Increased Nrf2 protein expression and nuclear translocation, increased LC3-II/LC3-I ratio, and increased autophagosome formation relative to SAH + vehicle controls.
Abolished protective effects on modified Garcia and beam balance scores, as well as changes in Nrf2, Keap1, p-SQSTM1, SQSTM1, and LC3-II/LC3-I levels when co-administered with mTOR activator MHY1485.
Abolished protective effects on modified Garcia and beam balance scores, as well as changes in Nrf2, Keap1, p-SQSTM1, SQSTM1, and LC3-II/LC3-I levels when co-administered with Nrf2 inhibitor ML385.

Animal Model:

C57BL/6 (male, 8 weeks old, subarachnoid haemorrhage model via stereotactic injection of autologous blood)^[1]
Dosage:

10 mg/kg/day
Administration:

p.o.; daily; 28 days
Result:

Reduced escape latency in the Morris water maze acquisition phase relative to SAH + vehicle controls.
Increased number of platform site crossings, increased time spent in the platform quadrant, and increased total distance travelled in the platform quadrant in the Morris water maze probe trial relative to SAH + vehicle controls.
Improved recognition index in the novel object recognition test relative to SAH + vehicle controls.
Improved preference index in the Y-maze test relative to SAH + vehicle controls.
Reduced number of FJC-positive degenerating neurons in the hippocampal CA1, CA3, and DG regions relative to SAH + vehicle controls.
Attenuated hippocampal neuronal shrinkage and death relative to SAH + vehicle controls.

Animal Model:

Sprague Dawley (adult male, 220-250 g, CLP-induced sepsis)^[5]
Dosage:

10 mg/kg; 30 mg/kg; 50 mg/kg
Administration:

i.p.; single dose
Result:

Significantly reduced serum cardiac troponin I (cTnI) levels and increased 7-day survival rate at 30 mg/kg and 50 mg/kg, with minimal effect at 10 mg/kg.
Significantly increased left ventricular ejection fraction (LVEF) and left ventricular fraction shortening (LVFS), decreased left ventricular end-systolic diameter (LVESD), and attenuated myocardial fiber disorder, edema, red blood cell exudation, and inflammatory cell infiltration at 30 mg/kg.
Reduced the number of TUNEL-positive cardiomyocytes, decreased BAX protein expression, and increased Bcl-2 protein expression at 30 mg/kg.
Improved mitochondrial ultrastructure (reduced swelling, cristae disruption, and vacuolation), increased myocardial ATP content, decreased dynamin-related protein 1 (DRP1) expression, suppressed mitochondrial ROS production, and increased superoxide dismutase 2 (SOD2) expression at 30 mg/kg.
Increased the number of myocardial autophagosomes, elevated the LC3II/LC3I ratio, and increased Beclin 1 protein expression at 30 mg/kg.
Abolished the anti-apoptotic effect (reduced TUNEL-positive cells, reduced BAX, increased Bcl-2) of 30 mg/kg when co-administered with autophagy inhibitor 3-methyladenine.

Animal Model:

C57BL/J mice (12 weeks old, 20.0 g; includes NG2-CreERT; Tau-mGFP transgenic mice and littermate controls)^[6]
Dosage:

10 mg/kg
Administration:

p.o.; daily; day 7 to day 28 post-microbead injection
Result:

Increased the number of CC1⁺ mature oligodendrocytes, Olig2⁺ total oligodendroglial lineage cells, and reduced the number of Tunel⁺/Olig2⁺ apoptotic oligodendroglial cells on day 28 compared to untreated glaucoma mice.
Increased myelinated axon numbers and improved myelin thickness (reduced G-ratio) in optic nerves on day 28 compared to untreated glaucoma mice.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 15686-51-8
Appearance Oil
Peso molecular 343.89
Fòrmula C₂₁H₂₆ClNO
Color Colorless to light yellow
SMILES

CN1[C@@H](CCO[C@](C2=CC=CC=C2)(C3=CC=C(Cl)C=C3)C)CCC1
Synonyms

HS-592; Meclastine
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (12)

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Journal Impact Factor

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 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 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 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 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.
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
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]

2024 Dec 3:115086. 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 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 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.
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
Res Sq

2026 Mar 23.
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 : 100 mg/mL (290.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9079 mL

14.5395 mL

29.0791 mL

5 mM

0.5816 mL

2.9079 mL

5.8158 mL

10 mM

0.2908 mL

1.4540 mL

2.9079 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Calculadora de dilución

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (289 KB)
SDS (254 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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OR (2659 KB)
SDS-PAGE (2659 KB)
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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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.9079 mL	14.5395 mL	29.0791 mL	72.6977 mL
	5 mM	0.5816 mL	2.9079 mL	5.8158 mL	14.5395 mL
	10 mM	0.2908 mL	1.4540 mL	2.9079 mL	7.2698 mL
	15 mM	0.1939 mL	0.9693 mL	1.9386 mL	4.8465 mL
	20 mM	0.1454 mL	0.7270 mL	1.4540 mL	3.6349 mL
	25 mM	0.1163 mL	0.5816 mL	1.1632 mL	2.9079 mL
	30 mM	0.0969 mL	0.4847 mL	0.9693 mL	2.4233 mL
	40 mM	0.0727 mL	0.3635 mL	0.7270 mL	1.8174 mL
	50 mM	0.0582 mL	0.2908 mL	0.5816 mL	1.4540 mL
	60 mM	0.0485 mL	0.2423 mL	0.4847 mL	1.2116 mL
	80 mM	0.0363 mL	0.1817 mL	0.3635 mL	0.9087 mL
	100 mM	0.0291 mL	0.1454 mL	0.2908 mL	0.7270 mL

Clemastine

12 Cited Publications

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Clemastine

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Publications Citing Use of MedChemExpress (MCE) Clemastine

Ver todos los productos específicos de isoformas Histamine Receptor

Ver todos los productos específicos de isoformas mAChR

Ver todos los productos específicos de isoformas mTOR

Ver todos los productos específicos de isoformas IKK

Actividad biológica

Chemical Information

Publications (12)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Clemastine Related Classifications

HY-B0298 Related Classifications