Clemastine Fumarate

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Cat Number

API14976579

CAS Number

14976-57-9

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CAS Number

14976-57-9

EINECS

239-055-2

Storage

2-8℃

Synonyms

(+)-2-(2-((p-chloro-alpha-methyl-alpha-phenylbenzyl)oxy)ethyl)-1-methylpyrro;1-methyl-2-(2-(methyl-p-chlorodiphenylmethyloxy)ethyl)pyrrolidine

Molecular Formula

C25H30ClNO5

Molecular Weight

459.96

Smiles

C[C@@](C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCC[C@H]3CCCN3C.C(=C/C(=O)O)\C(=O)O

Appearance

White to off-white solid

Melting Point

158-162℃

Relative Density

1.02

General Description

Clemastine Fumarate is a first-generation H1 receptor antagonist of the ethanolamine class. It is distinguished by potent antihistamine activity with relatively moderate sedative effects compared to other first-generation agents.

Mechanism of Action

Clemastine competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated allergic responses. It also crosses the blood-brain barrier, producing sedation through central H1 receptor antagonism.

Application

Used in the treatment of allergic conditions. Clemastine Fumarate is indicated for allergic rhinitis, urticaria, angioedema, and pruritic dermatoses requiring systemic antihistamine therapy.

Clemastine fumarate is an H1 receptor antagonist clinically used to treat allergic disorders. This study confirmed its efficacy against myocardial ischemia/reperfusion injury in a rat model of myocardial hypoxia/reperfusion. CLE reduced the expression of nerve growth factor-induced gene B (Nur77), glutamine-fructose-6-phosphate transaminase 2 (GFPT2), and C/EBP homologous protein (CHOP), decreased the area of myocardial infarction and the degree of endoplasmic reticulum stress. CLE pretreatment ameliorated abnormal fibers and myocardial edema and reduced the inflammatory cell infiltration caused by I/R injury. While Nur77 overexpression aggravated cardiac function, these effects were ameliorated by the downregulation of Nur77. These findings validate that CLE mitigates apoptosis and reduces endogenous stress within myocardial cells by modulating Nur77, GFPT2, and CHOP expression.

Fig. 1 Protein expression of GFPT2, Nur77 and CHOP. (He Y.; et al. 2025)

References

He Y, et al. Clemastine fumarate alleviates endoplasmic reticulum stress through the Nur77/GFPT2/CHOP pathway after ischemia/reperfusion in rat hearts. International immunopharmacology, 2025, 149: 114242.

Clemastine fumarate, distinct from its anti-allergic effect as an H1 histamine antagonist, has been identified as a promising drug for remyelination and autophagy enhancement in neurodegenerative diseases. The drug has been shown to cross the blood-brain barrier and act on specific neurons and neuroglia. Recent clinical trials, including the ReBUILD trial for multiple sclerosis, have demonstrated that clemastine promotes oligodendrocyte differentiation and myelin repair in chronic demyelinating injury.

Fig. 2 Clemastine fumarate for remyelination and autophagy enhancement in neurodegenerative diseases. (Zhu J.; et al. 2023)

References

Zhu J, et al. Drug repurposing: Clemastine fumarate and neurodegeneration. Biomedicine & Pharmacotherapy, 2023, 157: 113904.

What makes Clemastine preferable among first-generation antihistamines?

Clemastine provides potent antihistamine activity with relatively moderate sedation compared to other first-generation agents, offering a better tolerability balance.

What storage conditions are required?

Store at 2-8℃ in a tightly sealed container, protected from light and moisture.

What purity grade is available?

It is supplied as a high-purity grade suitable for R&D and pharmaceutical manufacturing.

Can packaging and order quantities be customized?

Yes, both packaging formats and order quantities can be tailored to meet specific R&D and production needs.