2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Autophagy Apoptosis NF-κB PI3K/Akt/mTOR
  3. Histamine Receptor mAChR Autophagy Apoptosis Keap1-Nrf2 p62 mTOR Pyroptosis IKK
  4. Clemastine

Clemastine  (Synonyms: HS-592; Meclastine)

Cat. No.: HY-B0298 Purity: 99.26%
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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.

For research use only. We do not sell to patients.

CAS No. : 15686-51-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 11 publication(s) in Google Scholar

Other Forms of Clemastine:

Clemastine Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

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    H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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    IKK-α IKK-β IKK IKKε TBK1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3][4][5][6].

    IC50 & Target

    H1 Receptor

     

    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.

    Clemastine Related Antibodies
    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.
    Clinical Trial
    Molecular Weight

    343.89

    Formula

    C21H26ClNO
    CAS No.
    Appearance

    Oil

    Color

    Colorless to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9079 mL 14.5395 mL 29.0791 mL
    5 mM 0.5816 mL 2.9079 mL 5.8158 mL
    View the 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. 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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    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      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.
    In Vivo Dissolution Calculator
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    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation
    References

    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. 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
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    Clemastine Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Clemastine15686-51-8HS-592 MeclastineHS592HS 592Histamine ReceptormAChRAutophagyApoptosisKeap1-Nrf2p62mTORPyroptosisIKKMuscarinic acetylcholine receptorSequestosome-1SQSTM1Mammalian target of RapamycinIκB kinaseI kappa B kinasep38 MAPK/NLRP3 signalingTHP-1 cellsHT-22 cellsH9c2 cardiomyocytesNrf2P2RX7muscarinic acetylcholine receptor M4CHRM1oligodendrocyte precursor cellhistamine H1 receptorInhibitorinhibitorinhibit

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