Clemastine (HS-592) fumarate

Catalog No.S1847 Synonyms: HS-592 fumarate, Meclastine fumarate

For research use only.

Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.

Clemastine (HS-592) fumarate Chemical Structure

CAS No. 14976-57-9

Selleck's Clemastine (HS-592) fumarate has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
mTOR [7] Histamine H1 receptor [1]
3 nM
In vitro

Clemastine 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] At concentrations of ≥25 μM, Clemastine Fumarate significantly blocks NK and ADCC reactions of lymphocytes against the human erythroleukemia cell line K562 and human B-lymphoblast cell line SB, respectively. [2] Clemastine Fumarate inhibits histamine-induced contraction of guinea pig ileum with an IC50 of 231 nM. [3] Clemastine Fumarate potently inhibits the HERG K+ channel in a concentration-dependent manner in HEK 293 cells stably expressing HERG channels with an IC50 of 12 nM, which can be attenuated by the Y652A or F656A mutation of HERG. [4] Clemastine Fumarate significantly potentiates ATP-induced increase in [Ca2+]i in HEKhP2X7 cells not relying on histamine receptor blockage but on sensitizing P2X7 receptor in a concentration-dependent manner with an EC50 of 10 μM, and increases the IL-1β release from LPS-induced human macrophages. [5]

In vivo

Administration of Clemastine Fumarate (5-20 mg/kg) displays significantly inhibitory effect on simultaneously induced zymosan paw oedema and croton oil ear oedema in rats in a dose-dependent manner, with the inhibition of 53.6% and 46.8%, respectively, at the dose of 20 mg/kg, and with ID50 values of 18.0 mg/kg and 20.5 mg/kg, respectively. [6] Clemastine Fumarate treatment strongly reduces innate immune responses to Listeria monocytogenes in mice by interfering with the extracellular signal-regulated kinase (ERK)-mediated production of proinflammatory cytokines such as TNF-α and IL-6 surprisingly not dependent on blocking the histamine H1 receptor, leading to significantly higher mortality. [7]

Protocol (from reference)

Animal Research:


  • Animal Models: Male Wistar rats with paw oedema induced by subplantar injection of zymosan and ear oedema induced by croton oil
  • Dosages: 5-20 mg/kg
  • Administration: Intraperitoneally

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 459.96


CAS No. 14976-57-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05359653 Not yet recruiting Drug: Clemastine Fumarate|Drug: Placebo Multiple Sclerosis (MS)|Multiple Sclerosis Relapsing-Remitting|Multiple Sclerosis Primary Progressive|Multiple Sclerosis Chronic Progressive|Multiple Sclerosis Relapse|Multiple Sclerosis Brain Lesion|Multiple Sclerosis Benign University of California San Francisco|United States Department of Defense May 1 2022 Phase 1|Phase 2
NCT05131828 Recruiting Drug: Metformin and clemastine in combination|Drug: Placebo Multiple Sclerosis Cambridge University Hospitals NHS Foundation Trust|University of Cambridge March 8 2022 Phase 2
NCT02040298 Completed Drug: Clemastine|Drug: Placebo Multiple Sclerosis Relapsing-Remitting University of California San Francisco January 2014 Phase 2
NCT01239719 Unknown status Drug: Dexamethasone + clemastine|Drug: Dexamethasone Allergy|Dermatitis Azidus Brasil March 2011 Phase 3

(data from, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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