Clemastine (HS-592) fumarate

Catalog No.S1847 Synonyms: Meclastine fumarate

For research use only.

Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.

Clemastine (HS-592) fumarate Chemical Structure

CAS No. 14976-57-9

Selleck's Clemastine (HS-592) fumarate has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Choose Selective Histamine Receptor Inhibitors

Other Histamine Receptor Products

Biological Activity

Description Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Targets
mTOR [7]
()
Histamine H1 receptor [1]
()
3 nM
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]

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 (from reference)

Animal Research:

[6]

  • Animal Models: Male Wistar rats with paw oedema induced by subplantar injection of zymosan and ear oedema induced by croton oil
  • Dosages: 5-20 mg/kg
  • Administration: Intraperitoneally
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 35 mg/mL warmed
(76.09 mM)
Water Insoluble
Ethanol Insoluble

* 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
Formula

C21H26ClNO.C4H4O4

CAS No. 14976-57-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05131828 Not yet recruiting Drug: Metformin and clemastine in combination|Drug: Placebo Multiple Sclerosis Cambridge University Hospitals NHS Foundation Trust|University of Cambridge February 2022 Phase 2
NCT02040298 Completed Drug: Clemastine|Drug: Placebo Multiple Sclerosis Relapsing-Remitting University of California San Francisco January 2014 Phase 2
NCT01239719 Unknown status Drug: Dexamethasone + clemastine|Drug: Dexamethasone Allergy|Dermatitis Azidus Brasil March 2011 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Clemastine (HS-592) fumarate | Clemastine (HS-592) fumarate ic50 | Clemastine (HS-592) fumarate price | Clemastine (HS-592) fumarate cost | Clemastine (HS-592) fumarate solubility dmso | Clemastine (HS-592) fumarate purchase | Clemastine (HS-592) fumarate manufacturer | Clemastine (HS-592) fumarate research buy | Clemastine (HS-592) fumarate order | Clemastine (HS-592) fumarate mouse | Clemastine (HS-592) fumarate chemical structure | Clemastine (HS-592) fumarate mw | Clemastine (HS-592) fumarate molecular weight | Clemastine (HS-592) fumarate datasheet | Clemastine (HS-592) fumarate supplier | Clemastine (HS-592) fumarate in vitro | Clemastine (HS-592) fumarate cell line | Clemastine (HS-592) fumarate concentration | Clemastine (HS-592) fumarate nmr