An internal standard for the quantification of carebastine
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Unlabeled Version(s)
23076Carebastine
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Carebastine-d5

Item No. 30755

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[4-(phenyl-d5)-phenylmethoxy)-1-piperidinyl]-1-oxobutyl]-α,α-dimethyl benzeneacetic acid
CAS Number
1189661-02-6
Molecular Formula
C32H32D5NO4
Formula Weight
504.7
Purity
≥99% deuterated forms (d1-d5)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: slightly solubleEthyl Acetate: slightly soluble
SMILES
O=C(C1=CC=C(C(C)(C)C(O)=O)C=C1)CCCN(CC2)CCC2OC(C3=CC=CC=C3)C4=C([2H])C([2H])=C([2H])C([2H])=C4[2H]
InChi Code
InChI=1S/C32H37NO4/c1-32(2,31(35)36)27-17-15-24(16-18-27)29(34)14-9-21-33-22-19-28(20-23-33)37-30(25-10-5-3-6-11-25)26-12-7-4-8-13-26/h3-8,10-13,15-18,28,30H,9,14,19-23H2,1-2H3,(H,35,36)/i3D,5D,6D,10D,11D
InChi Key
XGHOVGYJHWQGCC-KILXEUBNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $303

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    Product Description

    Carebastine-d5 is intended for use as an internal standard for the quantification of carebastine (Item No. 23076) by GC- or LC-MS. Carebastine is an active metabolite of ebastine (Item No. 15372) and a histamine H1 receptor antagonist (Ki = 75.86 nM).1,2,3 It inhibits histamine-induced contraction of isolated guinea pig trachea (IC50 = 120 nM).4 It also inhibits histamine release from isolated rat peritoneal mast cells and human basophils when used at concentrations ranging from 30 to 100 µM. Carebastine decreases production of chemokine (C-C motif) ligand 5 (CCL5) and CCL2 in human nasal epithelial cells isolated from patients with nasal allergies.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vincent, J., Liminana, R., Meredith, P.A., et al. The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects. Br. J. Clin. Pharmacol. 26(5), 497-502 (1988).

    2. Liu, K.-H., Kim, M.-G., Lee, D.-J., et al. Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: Major roles for CYP2J2 and CYP3A. Drug. Metab. Dispos. 34(11), 1793-1797 (2006).

    3. Hishinuma, S., Kosaka, K., Akatsu, C., et al. Asp73-dependent and -independent regulation of the affinity of ligands for human histamine H1 receptors by Na+. Biochem. Pharmacol. 128, 46-54 (2017).

    4. Yaku, I., Ishii, K., Seto, Y., et al. Pharmacological study of ebastine, a novel histamine H1-receptor antagonist. Nihon Yakurigaku Zasshi 103(3), 121-135 (1994).

    5. Yamauchi, Y., Fujikura, T., and Shimosawa, T. The effect of H1 antagonists carebastine and olopatadine on histamine induced expression of CC chemokines in cultured human nasal epithelial cells. Allergol. Int. 56(2), 171-177 (2007).