So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Zou, Ling; Pottel, Joshua; Khuri, Natalia; Ngo, Huy X.; Ni, Zhanglin; Tsakalozou, Eleftheria; Warren, Mark S.; Huang, Yong; Shoichet, Brian K.; Giacomini, Kathleen M. researched the compound: Sodium 6-hydroxy-5-((2-methoxy-5-methyl-4-sulfonatophenyl)diazenyl)naphthalene-2-sulfonate( cas:25956-17-6 ).Computed Properties of C18H14N2Na2O8S2.They published the article 《Interactions of Oral Molecular Excipients with Breast Cancer Resistance Protein, BCRP》 about this compound( cas:25956-17-6 ) in Molecular Pharmaceutics. Keywords: BCRP excipient; BCRP; drug−excipient interaction; excipient. We’ll tell you more about this compound (cas:25956-17-6).
Mechanistic-understanding-based selection of excipients may improve formulation development strategies for generic drug products and potentially accelerate their approval. Our study aimed at investigating the effects of mol. excipients present in orally administered FDA-approved drug products on the intestinal efflux transporter, BCRP (ABCG2), which plays a critical role in drug absorption with potential implications on drug safety and efficacy. We determined the interactions of 136 oral mol. excipients with BCRP in isolated membrane vesicles and identified 26 excipients as BCRP inhibitors with IC50 values less than 5 μM using 3H-cholecystokinin octapeptide (3H-CCK8). These BCRP inhibitors belonged to three functional categories of excipients: dyes, surfactants, and flavoring agents. Compared with noninhibitors, BCRP inhibitors had significantly higher mol. weights and SLogP values. The inhibitory effects of excipients identified in membrane vesicles were also evaluated in BCRP-overexpressing HEK293 cells at similar concentrations Only 1 of the 26 inhibitors of BCRP identified in vesicles inhibited BCRP-mediated 3H-oxypurinol uptake by more than 50%, consistent with the notion that BCRP inhibition depends on transmembrane or intracellular availability of the inhibitors. Collectively, the results of this study provide new information on excipient selection during the development of drug products with active pharmaceutical ingredients that are BCRP substrates.
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Reference:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics