An internal standard for the quantification of ketotifen
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Unlabeled Version(s)
20303Ketotifen (fumarate)
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Ketotifen-13C-d3

Item No. 28802

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1-(methyl-13C-d3)piperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
CAS Number
2748522-40-7
Molecular Formula
C18[13C]H16D3NOS
Formula Weight
313.4
Purity
≥99% deuterated forms (d1-d3)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: solubleDMF: solubleDMSO: solubleMethanol: soluble
SMILES
O=C1C2=C(C=CS2)/C(C3=CC=CC=C3C1)=C4CCN([13C]([2H])([2H])[2H])CC/4
InChi Code
InChI=1S/C19H19NOS/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19/h2-5,8,11H,6-7,9-10,12H2,1H3/i1+1D3
InChi Key
ZCVMWBYGMWKGHF-KQORAOOSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $436

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    Product Description

    Ketotifen-13C-d3 is intended for use as an internal standard for the quantification of ketotifen (Item No. 20303) by GC- or LC-MS. Ketotifen is a histamine H1 receptor antagonist (Ki = 1.3 nM) and mast cell stabilizer.1,2 It is selective for H1 receptors over H2 and H3 receptors (Kis = 987 and 2,500 nM, respectively).1 Ketotifen (50 and 100 μM) inhibits degranulation of rat peritoneal mast cells induced by compound 48/80 (Item No. 22173).2 It inhibits the passive cutaneous anaphylaxis (PCA) reaction in rats by 54.6% when administered orally at a dose of 20 mg/kg.3 Ketotifen (30 mg/kg) inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model.4 Formulations containing ketotifen have been used in the treatment of itching associated with allergic conjunctivitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sharif, N.A., Xu, S.X., and Yanni, J.M. Olopatadine (AL-4943A): Ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis. J. Ocul. Pharmacol. Ther. 12(4), 401-407 (1996).

    2. Baba, A., Tachi, M., Ejima, Y., et al. Anti-allergic drugs tranilast and ketotifen dose-dependently exert mast cell-stabilizing properties. Cell Physiol. Biochem. 38(1), 15-27 (2016).

    3. Nishikawa, Y., Shindo, T., Ishi, K., et al. Acrylamide derivatives as antiallergic agents. III. Synthesis and structure-activity relationships of N-[4-(4-diphenylmethyl-1-piperazinyl)butyl]- and N-[4-(4-diphenylmethylene-1-piperidyl)butyl]-3-heteroarylacry lamides. Chem. Pharm. Bull. (Tokyo) 37(3), 684-687 (1989).

    4. Miyagawa, N., Iwasaki, H., Kato, T., et al. Two pharmacological phases in antigen-induced immediate airway response in rats. Biol. Pharm. Bull. 32(12), 2260-2264 (2008).