Clemastine Fumarate
Catalog No.S1847
Molecular Weight(MW): 459.96
Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
Cited by 2 Publications
1 Customer Review
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(B,C) Analysis indicates the total distance was unchanged between cuprizone-exposed mice with or without clemastine treatment (B), but the distance in the central field decreased upon 6-week exposure to cuprizone, while clemastine gradually rescued the behavioral change (C). *P <0.05, n = 10 animals/group.
Neurosci Bull, 2015, 31(5):617-25. Clemastine Fumarate purchased from Selleck.
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Biological Activity
| Description | Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. | ||
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| Targets |
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| 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] |
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| 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] |
Protocol
| Animal Research:[6] |
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Solubility (25°C)
| In vitro | DMSO | 35 mg/mL warmed (76.09 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
5 mg/mL |
* 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.
Chemical Information
| Molecular Weight | 459.96 |
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| Formula | C21H26ClNO.C4H4O4 |
| CAS No. | 14976-57-9 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02521311 | Recruiting | Optic Neuritis | University of California San Francisco|Moorfields Eye Hospital NHS Foundation Trust | August 2016 | Phase 2 |
| NCT02613091 | Completed | Healthy Subjects | University of California San Francisco | April 2016 | Phase 1 |
| NCT02040298 | Completed | Multiple Sclerosis Relapsing-Remitting | University of California San Francisco | January 2014 | Phase 2 |
| NCT01239719 | Unknown status | Allergy|Dermatitis | Azidus Brasil | March 2011 | Phase 3 |
| NCT01125761 | Withdrawn | Dermatitis | Azidus Brasil | November 2010 | Phase 3 |
| NCT00481676 | Completed | Chronic Urticaria | Novartis | May 2007 | Phase 2 |
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