Home Neuronal Signaling Histamine Receptor antagonist - Autophagy activator - mTOR modulator Clemastine fumarate For research use only.

Clemastine fumarate

Synonyms: HS-592 fumarate, Meclastine fumarate

Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.

Clemastine fumarate Chemical Structure

Clemastine fumarate Chemical Structure

CAS No. 14976-57-9

Purity & Quality Control

Clemastine fumarate Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Targets
mTOR [7] Histamine H1 receptor [1]
3 nM
In vitro
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]
Kinase Assay Inhibition of [Ca2+]i
HL-60 cells are suspended at 1×107 cells/mL in a buffer consisting of 138 mM NaCl, 6 mM KC1, 1 mM MgSO4, 1 mM Na2HPO4, 5 mM NaHCO3, 5.5 mM glucose, and 20 mM HEPES-NaOH, pH 7.4, supplemented with 0.1% (w/v) bovine serum albumin. The dye fura-2/AM is added at a concentration of 4 μM, and cells are incubated for 10 minutes at 37 °C. Thereafter, cells are diluted with the aforementioned buffer to a concentration of 5×106 cells/mL and incubated for 45 minutes at 37 °C. Subsequently, cells are diluted with the aforementioned buffer to a final concentration of 0.5 × 106 cells/mL and centrifuged at 250 g for 10 minutes at 20 °C. Cells are suspended at 1.0 × 106 cells/mL in the aforementioned buffer and kept at 20 °C until measurement. HL-60 cells are used for up to 4 hours after loading with fura-2/AM, and suspended in 2 mL of the aforementioned buffer, using acryl fluorescence cuvettes. HL-60 cells are incubated for 3 minutes at 37 °C, in the presence of 1 mM Ca2+ and various concentrations of Clemastine Fumarate, before the addition of histamine (100 μM). Fluorescence is determined at 37 °C, with constant stirring of the cells at 1×103 rpm, using a Ratio II spectrofluorometer. The basal fluorescence (basal [Ca2+]i) is measured for 1 minute. The basal [Ca2+]i values are subtracted from the corresponding peak [Ca2+]i values, to calculate the increase in [Ca2+]i. The excitation and emission wavelengths are 340 and 500 nm, respectively. The IC50 value is assessed from competitive curve.
In Vivo
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]
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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06065670 Not yet recruiting
Demyelinating Diseases|Demyelination; Corpus Callosum|Multiple Sclerosis Brain Lesion|Multiple Sclerosis Acute and Progressive|Clinically Isolated Syndrome CNS Demyelinating
University of California San Francisco
 March 1 2024 Phase 1|Phase 2
NCT05359653 Recruiting
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
 August 1 2023 Phase 1|Phase 2
NCT05131828 Recruiting
Multiple Sclerosis
Cambridge University Hospitals NHS Foundation Trust|University of Cambridge
 March 8 2022 Phase 2
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

Chemical Information & Solubility

Molecular Weight 459.96 Formula

C21H26ClNO.C4H4O4
CAS No. 14976-57-9 SDF Download Clemastine fumarate SDF
Smiles CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 11 mg/mL ( (23.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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