MedChemExpress - Model Levocabastine -79516-68-0

Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].

Levocabastine

MCE China：Levocabastine

Brand：MedChemExpress (MCE)

Cat. No.HY-14277

CAS：79516-68-0

Synonyms：R 50547

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

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Description：Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).

In Vitro：Levocabastine (0-1000 μM; HEK-293 cells) causes inhibition of 125I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC50 of 406.2μm[3]. Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) inhibits α4β1 integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits α4β1 integrindependent adhesion of Jurkat cells to VCAM-1 with an IC50 of 395.6 μM, and the adhesion of EoL-1 cells with an IC50 of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC50=443.7 μM)[3].

In Vivo：Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) inhibits the virus-induced airway hyperresponsiveness[1]. Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) blocks anti-stress effect ofβ-LT on mouse behavior[2]. Levocabastine (500 µg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4[3].

IC50 & Target：H1 Receptor α4β1 NTR2 17 nM (Ki)

References：

[1]. Folkerts G, et, al. Virus-induced airway hyperresponsiveness in the guinea-pig: possible involvement of histamine and inflammatory cells. Br J Pharmacol. 1993 Apr;108(4):1083-93. [Content Brief]

[2]. Yamauchi R, et, al. Effect of beta-lactotensin on acute stress and fear memory. Peptides. 2006 Dec;27(12):3176-82. [Content Brief]

[3]. Qasem AR, et, al. Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62. [Content Brief]

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MedChemExpress - Model Levocabastine -79516-68-0

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Levocabastine