HPi1 是一种有口服活性的，针对幽门螺杆菌的选择性抗菌剂，IC50为 0.24 μM，MIC 为 0.08-0.16 μg/mL。

HPi1 is a selective and orally active antimicrobial against Helicobacter pylori (IC50: 0.24 μM and a MIC of 0.08-0.16 μg/mL). HPi1 is inactive against other Xaliproden, including the gut commensals, Lactobacillus reuteri, Lactobacillus casei, and Bifidobacterium longum.

HPi1 is effective against the clarithromycin-resistant strains ARHp172 (MIC of 0.004–0.016 μg/mL) and ARHp246 (MIC of 0.008–0.032 μg/mL). HPi1 has some activity against the Bacteroides species, but at concentrations at least 18-fold higher than the H. pylori MIC. HPi1 has good physicochemical and pharmacological properties, including determining the aqueous solubility (19 μg/mL), human plasma protein binding (93% bound), stability with human liver microsomes (T1/2 of 1.3 hours), and the ability to passively permeate membranes. The MIC against H. pylori isolates ranged from 0.002-0.032 μg/mL (0.01-0.17 μM) in the agar dilution assay. More potent activity is detected for Campylobacter jejuni with a MIC of 0.3 μg/mL.

Treated with HPi1 (6.25-50 mg/kg; Oral gavage; once a day; for 3 days; female C57BL/6 mice), reduces colony counts below the limit of detection at doses of 25 or 50 mg/kg/day.

13080-21-2

C8H8N4S

192.24

DMSO:60 mg/mL (312.11 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years