Triclabendazole sulfoxide

产品说明书

Print
Chemical Structure| 100648-13-3 同义名 : TCBZ-SO
CAS号 : 100648-13-3
货号 : A906988
分子式 : C14H9Cl3N2O2S
纯度 : 97%
分子量 : 375.658
MDL号 : MFCD19441813
存储条件:

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Triclabendazole sulfoxide (TCBZSO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. TCBZSO is ABCG2 inhibitor. TCBZSO administration also inhibited nitrofurantoin Abcg2-mediated secretion into milk by more than 2-fold and increased plasma levels of the sulfonamide sulfasalazine by more than 1.5-fold in mice[1]. CYP1A2, CYP2C8, CYP2C9 were inhibited by triclabendazole sulfoxide with IC50 of 4.19 µM, 8.95 µM, and 1.95 µM, respectively. CYP2C19 was inhibited by triclabendazole and triclabendazole sulfoxide with IC50 of 0.25 and 0.22 µM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.31mL

2.66mL

1.33mL

26.62mL

5.32mL

2.66mL

参考文献

[1]Barrera B, Otero JA, Egido E, Prieto JG, Seelig A, Álvarez AI, Merino G. The anthelmintic triclabendazole and its metabolites inhibit the membrane transporter ABCG2/BCRP. Antimicrob Agents Chemother. 2012 Jul;56(7):3535-43

[2]Giri P, Gupta L, Naidu S, Joshi V, Patel N, Giri S, Srinivas NR. In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole, Aldicarb, Methiocarb, Montelukast and Ziprasidone. Drug Metab Lett. 2018;12(2):101-116