Bepotastine Besilate

• CAT Number: A000247
• CAS Number: 190786-44-8
• Molecular Formula: C27H31ClN2O6S
• Molecular Weight: 547.06
• Purity: ≥95%
• Target: Histamine Receptor
• Solubility: Soluble in DMSO > 10 mM
• Storage: 0 - 4 °C for short term or -20 °C for long term
• IUPAC Name: benzenesulfonic acid;4-[4-[(S)-(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
• InChI: InChI=1S/C21H25ClN2O3.C6H6O3S/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26;7-10(8,9)6-4-2-1-3-5-6/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26);1-5H,(H,7,8,9)/t21-;/m0./s1
• InChIKey: UDGHXQPQKQPSBB-BOXHHOBZSA-N
• SMILES: C1CN(CCC1OC(C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O.C1=CC=C(C=C1)S(=O)(=O)O

Bepotastine Besilate (CAS 190786-44-8) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. It was approved in Japan for use in the treatment of allergic rhinitis and urticaria/pruritus in July 2000 and January 2002, respectively.

Overview of Clinical Research

Bepotastine Besilate is a histamine H1 receptor antagonist. It has been granted for the new molecular entity. 

Dong-A ST completed a phase I trial in Healthy volunteers in South Korea (NCT03932435) in 2020.

Reference

1: Okubo K, Ichimura M, Koyama T, Susuta Y, Izaki H. Double-blind placebo-controlled study of bepotastine besilate in pediatric patients with perennial allergic rhinitis. Expert Opin Pharmacother. 2015;16(16):2395-408. doi: 10.1517/14656566.2015.108