Clemastine Fumarate

Catalog No.S1847

Clemastine Fumarate Chemical Structure

Molecular Weight(MW): 459.96

Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

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In DMSO USD 130 In stock
USD 97 In stock
USD 970 In stock
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1 Customer Review

  • (B,C) Analysis indicates the total distance was unchanged between cuprizone-exposed mice with or without clemastine treatment (B), but the distance in the central field decreased upon 6-week exposure to cuprizone, while clemastine gradually rescued the behavioral change (C). *P <0.05, n = 10 animals/group.

    Neurosci Bull, 2015, 31(5):617-25. Clemastine Fumarate purchased from Selleck.

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Biological Activity

Description Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
Targets
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

Animal Research:[6]
+ Expand
  • Animal Models: Male Wistar rats with paw oedema induced by subplantar injection of zymosan and ear oedema induced by croton oil
  • Formulation: Dissolved in saline
  • Dosages: 5-20 mg/kg
  • Administration: Intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL warmed (76.09 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 459.96
Formula

C21H26ClNO.C4H4O4

CAS No. 14976-57-9
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02521311 Recruiting Optic Neuritis University of California, San Francisco August 2016 Phase 2
NCT02613091 Completed Healthy Subjects University of California, San Francisco April 2016 Phase 1
NCT02040298 Completed Multiple Sclerosis, Relapsing-Remitting University of California, San Francisco January 2014 Phase 2
NCT01239719 Unknown status Allergy|Dermatitis Azidus Brasil March 2011 Phase 3
NCT01125761 Withdrawn Dermatitis Azidus Brasil November 2010 Phase 3
NCT00481676 Completed Chronic Urticaria Novartis May 2007 Phase 2

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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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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID