Clemastine (HS-592) Fumarate

製品コードS1847 バッチS184705

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	92 mg/mL (200.01 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Clemastine fumarateは、IC50 3 nMの選択的histamine H1受容体拮抗薬です。ClemastineはmTOR経路を介してautophagyを刺激します。
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. 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. Clemastine Fumarate inhibits histamine-induced contraction of guinea pig ileum with an IC50 of 231 nM. 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. 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.
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. 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.

製品説明

Clemastine fumarateは、IC50 3 nMの選択的histamine H1受容体拮抗薬です。ClemastineはmTOR経路を介してautophagyを刺激します。

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.

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.

Clemastine Fumarate inhibits histamine-induced contraction of guinea pig ileum with an IC50 of 231 nM.

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.

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.

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.

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.

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
Clemastine ameliorates cognitive deficits in an experimental rat model of chronic cerebral hypoperfusion [ J Cereb Blood Flow Metab, 2025, 0271678X251382874]	PubMed: 41185380
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

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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