Structure of Clemastine fumarate
CAS No.: 14976-57-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
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 << |
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.
|
Tags: Clemastine | HS-592 | Meclastine | HS592 | HS 592 | Histamine Receptor | antihistamine | H1 receptor | anti-inflammatory | H1 receptor antagonist | antihistamine | allergic reaction relief | 14976-57-9
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