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Synonyms | HS-592 fumarate, Meclastine fumarate | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H26ClNO.C4H4O4 |
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分子量 | 459.96 | CAS No. | 14976-57-9 | |
Solubility (25°C)* | 体外 | DMSO | 15 mg/mL warmed with 50ºC water bath (32.61 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. |
製品説明 | Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway. |
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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] |
キナーゼアッセイ | Inhibition of [Ca2+]i | |
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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. | ||
細胞アッセイ | 細胞株 | H9c2 cardiomyocytes |
濃度 | 1.25 ug/ml | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | Male Wistar rats with paw oedema induced by subplantar injection of zymosan and ear oedema induced by croton oil |
投薬量 | 5-20 mg/kg | |
投与方法 | Intraperitoneally |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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