Clemastine fumarate

Catalog No.S1847 Batch:S184704

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Technical Data

Formula

C21H26ClNO.C4H4O4

Molecular Weight 459.96 CAS No. 14976-57-9
Solubility (25°C)* In vitro DMSO 30 mg/mL (65.22 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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)

Kinase Assay:

[1]

  • 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.

Animal Study:

[6]

  • 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

Customer Product Validation

Data from [Data independently produced by , , Front Cell Neurosci, 2018, 12:412]

Data from [Data independently produced by , , Neurosci Bull, 2015, 31(5):617-25]

Selleck's Clemastine fumarate has been cited by 15 publications

Clemastine-induced enhancement of hippocampal myelination alleviates memory impairment in mice with chronic pain [ Neurobiol Dis, 2024, 190:106375] PubMed: 38092269
The Eph receptor A4 plays a role in demyelination and depression-related behavior [ J Clin Invest, 2022, e152187] PubMed: 35271507
Clemastine Promotes Differentiation of Oligodendrocyte Progenitor Cells Through the Activation of ERK1/2 via Muscarinic Receptors After Spinal Cord Injury [ Front Pharmacol, 2022, 13:914153] PubMed: 35865954
Clemastine Rescues Chemotherapy-Induced Cognitive Impairment by Improving White Matter Integrity [ Neuroscience, 2022, S0306-4522(22)00001-X] PubMed: 35007691
Enhancing myelin renewal reverses cognitive dysfunction in a murine model of Alzheimer's disease [ Neuron, 2021, S0896-6273(21)00352-4] PubMed: 34102111
Chronic Exposure to Hypoxia Inhibits Myelinogenesis and Causes Motor Coordination Deficits in Adult Mice [ Neurosci Bull, 2021, 10.1007/s12264-021-00745-1] PubMed: 34292513
Clemastine Enhances Myelination, Delays Axonal Loss and Promotes Functional Recovery in Spinal Cord Injury [ Neurochem Res, 2021, 10.1007/s11064-021-03465-0] PubMed: 34661796
Myelin degeneration and diminished myelin renewal contribute to age-related deficits in memory. [ Nat Neurosci, 2020, 10.1038/s41593-020-0588-8] PubMed: 32042174
Extrinsic immune cell-derived, but not intrinsic oligodendroglial factors contribute to oligodendroglial differentiation block in multiple sclerosis [ Acta Neuropathol, 2020, 140(5):715-736] PubMed: 32894330
Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms. [ Anticancer Res, 2019, 39(7):3767-3775] PubMed: 31262903

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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