Molecular Weight(MW): 459.96
Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
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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.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|Description||Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.|
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. |
-  Seifert R, et al. Mol Pharmacol, 1992, 42(2), 227-234.
-  Nair MP, et al. Cell Immunol, 1983, 81(1), 45-60.
-  Merlos M, et al. J Pharmacol Exp Ther, 1997, 280(1), 114-121.
|In vitro||DMSO||35 mg/mL warmed (76.09 mM)|
|In vivo||Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
* 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.
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02521311||Recruiting||Optic Neuritis||University of California, San Francisco||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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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