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Clemastine (fumarate) (CAS 14976-57-9) LS-H102

Histamin H1 receptor antagonist
LS-H102-100 / 100 mg / $195
LS-H102-250 / 250 mg / $225
LS-H102-500 / 500 mg / $285
LS-H102-1000 / 1000 mg / $395
USA Shipment Only
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Description: Clemastine is a selective histamine H1 receptor antagonist (Ki = 0.26 nM) that also displays high affinity for muscarinic receptors (Ki = 16 nM). It has also recently been identified as a positive allosteric modulator of P2X7 receptor signaling. Clemastine has long been used to inhibit histamine-induced bronchoconstriction in asthma and airway hyperresponsive studies. H102_ChemicalStructureImage.png
?(2R)-2-[2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methyl-pyrrolidine, 2E-butenedioate?
 
biochemical, chemical, antagonist
LS-H102
14976-57-9
C21H26ClNO • C4H4O4
≥98%
A crystalline solid
0
ClC1=CC=C([C@@](OCC[C@H]2CCCN2C)(C)C3=CC=CC=C3)C=C1.OC(/C=C/C(O)=O)=O
InChI=1S/C21H26ClNO.C4H4O4/c1-21(17-7-4-3-5-8-17,18-10-12-19(22)13-11-18)24-16-14-20-9-6-15-23(20)2;5-3(6)1-2-4(7)8/h3-5,7-8,10-13,20H,6,9,14-16H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t20-,21-;/m1./s1
PMGQWSIVQFOFOQ-YKVZVUFRSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: HRH1 / Histamine H1 Receptor related products

Usage Information

Clemastine (fumarate) is supplied as a crystalline solid. A stock solution may be made by dissolving the clemastine (fumarate) in the solvent of choice. Clemastine (fumarate) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of clemastine (fumarate) in these solvents is approximately 0.1, 2.5, and 1.6 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of clemastine (fumarate) can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of clemastine (fumarate) in PBS, pH 7.2, is approximately 0.3 mg/ml. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Kubo, N., Shirakawa, S., Kuno, T., et al. Antimuscarinic effects of antihistamines: Quantitative evaluation by receptor-binding assay. Jpn. J. Pharmacol. 43(3), 277-282 (1987).
  2. Nörenberg, W., Hempel, C., Urban, N., et al. Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations. J. Biol. Chem. 286(13), 11067-11081 (2011).
  3. Hartman, V., Magnussen, H., Holle, J.P., et al. Modulation of histamine-induced bronchoconstriction with inhaled, oral, and intravenous clemastine in normal and asthmatic subjects. Thorax 36(10), 737-740 (2013).

 


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