A histamine H1 receptor antagonist
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Clemastine (fumarate)

Item No. 14637

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-2-[2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methyl-pyrrolidine, 2E-butenedioate
CAS Number
14976-57-9
Molecular Formula
C21H26ClNO • C4H4O4
Formula Weight
460.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1.6 mg/mlDMSO: 2.5 mg/mlEthanol: 0.1 mg/mlPBS (pH 7.2): 0.3 mg/ml
SMILES
ClC1=CC=C([C@@](OCC[C@H]2CCCN2C)(C)C3=CC=CC=C3)C=C1.OC(/C=C/C(O)=O)=O
InChi Code
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
InChi Key
PMGQWSIVQFOFOQ-YKVZVUFRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 mg

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    Cayman Chemical
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    Product Description

    Clemastine is a histamine H1 receptor antagonist (Ki = 0.26 nM).1 It is selective for the histamine H1 receptor over muscarinic acetylcholine receptors (mAChRs; Ki = 16 nM), as well as over sigma-1 (σ1) and σ2 and α2A-, α2B-, and α2C-adrenergic receptors (Kis = 67, 15, 1,365, 691, and 545 nM, respectively).1,2 Clemastine (0.12 mg/kg) alone or in combination with the histamine H2 receptor antagonist cimetidine (Item No. 18743) reduces ovalbumin-induced bronchial obstruction in ovalbumin-sensitized guinea pigs.3 It also decreases severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 0.95 µM) with a 50% cytotoxic concentration (CC50) value of >20 µM.4 Formulations containing clemastine have been used in the treatment of allergic rhinitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. Gregori-Puigjané, E., Setola, V., Hert, J., et al. Identifying mechanism-of-action targets for drugs and probes. Proc. Natl. Acad. Sci. USA 109(28), 11178-11183 (2012).

    3. Dorsch, W., Reimann, H.J., and Neuhauser, J. Histamine1--histamine2 antagonism: Effect of combined clemastine and cimetidine pretreatment on allergen and histamine-induced reactions of the guinea pig lung in vivo and in vitro. Agents Actions 12(1-2), 113-118 (1982).

    4. Yang, L., Pei, R.-J., Li, H., et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol. Sin. 42(8), 1347-1353 (2020).