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Chemical Structure| 14976-57-9 Chemical Structure| 14976-57-9

Structure of Clemastine fumarate
CAS No.: 14976-57-9

Chemical Structure| 14976-57-9

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Clemastine fumarate is a selective antagonist of histamine H1 receptor with IC50 of 3 nM.

Synonyms: HS-592 fumarate; Meclastine fumarate; Clemastine (fumarate)

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Product Details of Clemastine fumarate

CAS No. :14976-57-9
Formula : C25H30ClNO5
M.W : 459.96
SMILES Code : CN1[C@@H](CCO[C@](C2=CC=CC=C2)(C3=CC=C(Cl)C=C3)C)CCC1.O=C(O)/C=C/C(O)=O
Synonyms :
HS-592 fumarate; Meclastine fumarate; Clemastine (fumarate)
MDL No. :MFCD00137486
InChI Key :PMGQWSIVQFOFOQ-YKVZVUFRSA-N
Pubchem ID :5281069

Safety of Clemastine fumarate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Clemastine fumarate

GPCR

Isoform Comparison

Biological Activity

Target
  • H1 receptor

    Histamine H1 receptor, IC50:3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Microglial cells 20 ng/mL 1 hour Clemastine inhibited the upregulation of IL-1β and NLRP3 in microglial cells induced by OGD. PMC7023767
Plasmodium falciparum 3D7 10 μM 12-72 hours To evaluate the inhibitory effect of clemastine on Plasmodium growth, results showed that 10 μM clemastine completely inhibited parasite loads in blood and liver cells. PMC7084109
Huh-7 cells 20 µM 2 days Screening for SARS-CoV-2 virus entry inhibitors, Clemastine showed the strongest anti-SARS2 activity (EC50=0.95 ± 0.83 µM). PMC7594953
Vero E6 cells 10 µM 24 hours Validation of Clemastine's inhibitory effect on native SARS-CoV-2 virus, showing significant inhibition of viral replication. PMC7594953
Rat oligodendrocyte precursor cells 1 μM 3 days To evaluate the effect of Clemastine on oligodendrocyte precursor cell differentiation and myelination. Results showed that Clemastine significantly enhanced oligodendrocyte differentiation and myelination. PMC4830134
Oligodendrocyte precursor cells (OPCs) 1 µM 5 days Promotes oligodendrocyte precursor cell maturation and central nervous system myelination PMC10739966
Oligodendrocyte precursor cells (OPCs) 1 μM 7 days Clemastine treatment reduced excess oligodendrocyte precursor cells and normalized oligodendrocyte density. PMC10393406
Oligodendrocyte progenitor cells (OPCs) 20 ng/mL 7 days Clemastine reversed the inhibition of IL-1β on OPC maturation and promoted the expression of MBP and CNPase. PMC7023767
Oligodendrocyte precursor cells co-cultured with dorsal root ganglion neurons 500 nM To evaluate the effect of Clemastine on myelination in a co-culture system. Results showed that Clemastine significantly promoted myelination. PMC4830134
Huh7 hepatocytes 10 μM To evaluate the cytotoxicity of clemastine on human hepatocytes, results showed that 10 μM clemastine did not exhibit cytotoxicity. PMC7084109

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Bilateral common carotid artery occlusion (BCCAO) model Intraperitoneal injection 1 mg/kg 14 consecutive days Clemastine improved hypomyelination in BCCAO rats and restrained the upregulation of IL-1β and NLRP3. PMC7023767
Mice Murine neonatal hypoxic injury model Oral gavage 10 mg/kg Once daily from postnatal Days 3–10 Promotes oligodendrocyte precursor cell differentiation, myelination, and functional recovery PMC6394402
Mice Experimental autoimmune encephalomyelitis (EAE) Oral 10 mg/kg Once daily for 28 days To evaluate the remyelination efficacy of Clemastine in the EAE model, results showed that Clemastine improved VEP latency and increased the number of remyelinated axons in the optic nerve. PMC10200282
Mice Fear memory model Intraperitoneal injection 10 mg/kg Once daily from 3 days pre-conditioning to 21 days post-conditioning Promotes new myelin formation, improves remote memory recall and promotes fear generalization PMC7213814
Mice Anks1b-deficient mouse models Intraperitoneal injection 10 mg/kg Daily for 14 days Rescues deficits in social preference in Anks1b-deficient mice PMC10739966
Mice Cuprizone-mediated demyelination model Gavage 10 mg/kg Once daily for three weeks Clemastine enhances oligodendrocyte gain during remyelination but is less effective than LL-341070, failing to fully eliminate the regeneration deficit after severe demyelination. PMC11739692
C57BL/6J mice Chronic microelectrode implantation model Intraperitoneal injection 10 mg/kg Daily administration for 16 weeks Clemastine administration significantly elevated the signal detectability and quality, rescued the loss of multi-unit activity, and increased functional interlaminar connectivity over 16-weeks of implantation. Additionally, post-mortem immunohistochemistry showed that increased oligodendrocyte density and myelination coincided with increased survival of both excitatory and inhibitory neurons near the implant. PMC10528716
Mice Pitt–Hopkins syndrome mouse model Intraperitoneal injection 10 mg/kg Once daily for 14 days Clemastine treatment normalized oligodendrocyte precursor cell and oligodendrocyte density and increased the number of axons undergoing myelination. PMC10393406
Rat Neonatal hypoxic-ischemic brain injury model Intraperitoneal injection 10 mg/kg Once daily for 6 consecutive days Clemastine promotes oligodendrocyte proliferation through the MAPK/ERK pathway, reduces white matter injury, and exhibits neuroprotective effects. PMC11311837
Mice Chronic hypoxia model Oral gavage 10 mg/kg per day Once daily from P3 to P10 Enhancing myelination and promoting functional recovery PMC6170028
C57BL/6 mice Cuprizone-induced mouse model of demyelination Oral 10 mg/kg per day Daily for 3 weeks Clemastine treatment greatly enhanced myelin repair in the demyelinated regions with increased mature oligodendrocytes (APC-positive) and myelin basic protein. More importantly, compared to vehicle, clemastine treatment rescued the schizophrenia-like behavioral changes in the open field test and the Y-maze, suggesting a beneficial effect via promoting myelin repair. PMC5563681
Mice Toxic injury model in spinal cord white matter tracts Oral gavage 10 mg/kg/day Once daily for 14 days To evaluate the effect of Clemastine on remyelination. Results showed that Clemastine significantly accelerated the kinetics of remyelination and reduced the proportion of unmyelinated axons. PMC4830134
Mice C57BL/6 mice Oral 10 mg/kg/day Once daily for 4 months Enhanced myelination and improved spatial memory in aged mice PMC7306053
Mice APP/PS1 transgenic mouse model Oral 10 mg/kg/day Daily for 3 months Enhancing myelination to improve memory-related task performance and hippocampal sharp wave ripples in APP/PS1 mice PMC8298291
Plasmodium berghei ANKA Liver-stage malaria model Not specified 10 μM Not specified To evaluate the inhibitory effect of clemastine on liver-stage Plasmodium, results showed that 10 μM clemastine completely inhibited parasite loads in liver cells. PMC7084109
Xenopus laevis tadpoles Tg(mbp:GFP-NTR) transgenic model Water solution administration 200 nM 3 days To evaluate the effect of Clemastine on promoting remyelination, results showed that the number of GFP+ oligodendrocytes in the clemastine-treated group was 1.5-fold higher than the control group, and the visual avoidance index improved by 1.4-fold. PMC10232271

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01154361 Angioedema Phase 2 Completed - Germany ... More >> Klinikum rechts der Isar Hals-Nasen-Ohrenklinik der TUM Munich, Bavaria, Germany, 81675 Less <<
NCT00481676 - Completed - -
NCT01125761 Dermatitis Phase 3 Withdrawn - Brazil ... More >> LAL Clinica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 LAL Clínica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 Less <<
NCT00913549 Allergy Phase 1 Completed - -
NCT02613091 Healthy Subjects PHASE1 COMPLETED - Sandler Neurosciences Building... More >>, Neurological Clinical Research Unit, San Francisco, California, 94107, United States Less <<
NCT00481676 Chronic Urticaria Phase 2 Completed - Germany ... More >> Novartis Investigative Site Berlin, Germany Novartis Investigative Site Bonn, Germany Novartis Investigative Site Dresden, Germany Novartis Investigative Site Giessen, Germany Novartis Investigative Site Hamburg, Germany Novartis Investigative Site Hannover, Germany Novartis Investigative Site Koeln, Germany Novartis Investigative Site Leipzig, Germany Novartis Investigative Site Luebeck, Germany Novartis Investigative Site Mainz, Germany Novartis Investigative Site Munich, Germany Less <<
NCT02521311 Optic Neuritis Phase 2 Recruiting January 2021 United States, California ... More >> University of California San Francisco Recruiting San Francisco, California, United States, 94158 Contact: Tracy Tran, BA    415-353-2707    tracy.tran@ucsf.edu Less <<
NCT02040298 Multiple Sclerosis, Relapsing-... More >>Remitting Less << Phase 2 Completed - United States, California ... More >> UCSF Multiple Sclerosis Center San Francisco, California, United States, 94518 Less <<
NCT01239719 Allergy Derma... More >>titis Less << Phase 3 Unknown December 2011 -
NCT01257061 Eczema Phase 3 Unknown August 2013 Brazil ... More >> Medcin instituto da Pele Recruiting Osasco, São Paulo, Brazil, 060323-000 Contact: Flavia Addor    5511 3681 6362 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.87mL

2.17mL

1.09mL

21.74mL

4.35mL

2.17mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

Historical Records

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