Clemastine fumarate

製品コードS1847 バッチS184706

印刷

化学情報

Synonyms

HS-592 fumarate, Meclastine fumarate

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₂₆ClNO.C₄H₄O₄

分子量

459.96

CAS No.

14976-57-9

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

15 mg/mL (32.61 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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

製品説明

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

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]

プロトコル(参考用のみ)

キナーゼアッセイ	Inhibition of [Ca²⁺]_i
キナーゼアッセイ	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

参考

https://pubmed.ncbi.nlm.nih.gov/1381043/
https://pubmed.ncbi.nlm.nih.gov/6225527/
https://pubmed.ncbi.nlm.nih.gov/8996188/

https://pubmed.ncbi.nlm.nih.gov/16288909/
https://pubmed.ncbi.nlm.nih.gov/21262970/
https://pubmed.ncbi.nlm.nih.gov/9149318/
https://europepmc.org/article/ppr/ppr181381
https://pubmed.ncbi.nlm.nih.gov/35274595/

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カスタマーフィードバック

: 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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

SGK1 drives hippocampal demyelination and diabetes-associated cognitive dysfunction in mice [ Nat Commun, 2025, 16(1):1709]	PubMed: 39962079
Hypomyelination in autism-associated neuroligin-3 mutant mice impairs parvalbumin interneuron excitability, gamma oscillations, and sensory discrimination [ Nat Commun, 2025, 16(1):6382]	PubMed: 40640134
Clemastine enhances myelin formation in the striatum and medial prefrontal cortex and improves sociability in a neonatal rat hypoxic-ischemic model [ Biomed Pharmacother, 2025, 185:117916]	PubMed: 40058153
Evaluating the effects of pro-myelinating drugs on motor function and myelination in a zebrafish model of genetic leukoencephalopathy [ Neurosci Lett, 2025, 862:138280]	PubMed: 40456507
Pharmacogenomic screening identifies and repurposes leucovorin and dyclonine as pro-oligodendrogenic compounds in brain repair [ Nat Commun, 2024, 15(1):9837]	PubMed: 39537633
The paracaspase MALT1 controls cholesterol homeostasis in glioblastoma stem-like cells through lysosome proteome shaping [ Cell Rep, 2024, 43(1):113631]	PubMed: 38183651
Remyelination-oriented clemastine treatment attenuates neuropathies of optic nerve and retina in glaucoma [ Glia, 2024, 72(9):1555-1571]	PubMed: 38829008
Clemastine-induced enhancement of hippocampal myelination alleviates memory impairment in mice with chronic pain [ Neurobiol Dis, 2024, 190:106375]	PubMed: 38092269
Minimum effective dose of clemastine in a mouse model of preterm white matter injury [ Pediatr Res, 2024, 96(4):933-941]	PubMed: 38942888
Prophylactic clemastine treatment improves influenza A virus-induced cognitive dysfunction in mice [ Brain Behav Immun Health, 2024, 42:100891]	PubMed: 39881819

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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