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

Clemastine fumarate  (Synonyms: HS-592 fumarate; Meclastine fumarate)

Cat. No.: HY-B0298A Purity: 99.96%
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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 .

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

CAS No. : 14976-57-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Clemastine fumarate:

Clemastine fumarate Related Antibodies

Top Publications Citing Use of Products

    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.

    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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    H1 Receptor

     

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    0.951 μM
    Compound: 92125238
    HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
    HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
    		[PMID: 22586124]
    HepG2 IC50
    > 50 μM
    Compound: 92125238
    HARVARD: Cytotoxicity in HepG2 cell line
    HARVARD: Cytotoxicity in HepG2 cell line
    		[PMID: 22586124]
    Huh-7 CC50
    > 100 μM
    Compound: Clemastine fumarate
    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
    		[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.

    Clemastine fumarate Related Antibodies
    Molecular Weight

    459.96

    Formula

    C25H30ClNO5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1741 mL 10.8705 mL 21.7410 mL
    5 mM 0.4348 mL 2.1741 mL 4.3482 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, 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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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: ≥ 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.
    • Protocol 2

      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.

    • Protocol 1

      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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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).

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    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

    Purity: 99.96%

    SDS (396 KB)

    COA (258 KB) HNMR (278 KB) RP-HPLC (248 KB) MS (71 KB)

    Handling Instructions (2659 KB)
    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, 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.

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    Clemastine fumarate 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:

    Clemastine14976-57-9HS-592MeclastineHS592HS 592p62PyroptosisAutophagyKeap1-Nrf2mTORmAChRHistamine ReceptorIKKApoptosisSequestosome-1SQSTM1Mammalian target of RapamycinMuscarinic acetylcholine receptorIκB kinaseI kappa B kinase antihistamineH1 receptoranti-inflammatoryoralallergic reactionsInhibitorinhibitorinhibit

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