HPi1 

HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC₅₀ of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum^[1].

IC50: 0.24 μM (Helicobacter pylori)^[1]
MIC: 0.08-0.16 μg/mL (Helicobacter pylori)^[1]

The MIC against H. pylori isolates ranged from 0.002-0.032 μg/mL (0.01-0.17 μM) in the agar dilution assay. 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)^[1].
HPi1 has some activity against the Bacteroides species, but at concentrations at least 18-fold higher than the H. pylori MIC. More potent activity is detected for Campylobacter jejuni with an MIC of 0.3 μg/mL^[1].
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 (T_1/2 of 1.3 hours) and the ability to passively permeate membranes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HPi1 (6.25-50 mg/kg; Oral gavage; once a day; for 3 days; female C57BL/6 mice) treatment decreases colony counts below the limit of detection at doses of 25 or 50 mg/kg/day^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

192.24

Solid

C₈H₈N₄S

13080-21-2

S=C1NC2=C(C=CC=C2)N=C1NN

Room temperature in continental US; may vary elsewhere.

• [1]. Gavrish E, et al. In vitro and in vivo activities of HPi1, a selective antimicrobial against Helicobacter pylori. Antimicrob Agents Chemother. 2014 Jun;58(6):3255-60.  [Content Brief]