| Name | HPi1 |
| Description | 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. |
| In vitro | HPi1 demonstrates efficacy against clarithromycin-resistant H. pylori strains ARHp172 (with a minimum inhibitory concentration (MIC) of 0.004–0.016 μg/mL) and ARHp246 (MIC of 0.008–0.032 μg/mL). Although HPi1 is somewhat effective against Bacteroides species, the required concentration is significantly higher (at least 18 times) than for inhibiting H. pylori. The compound possesses favorable physicochemical and pharmacological characteristics, including an aqueous solubility of 19 μg/mL, 93% human plasma protein binding, a half-life of 1.3 hours in the presence of human liver microsomes, and the capacity for passive membrane permeation. Its MIC values against various H. pylori isolates range from 0.002 to 0.032 μg/mL (0.01 to 0.17 μM) according to agar dilution assays, indicating broad activity. Additionally, HPi1 exhibits even stronger activity against Campylobacter jejuni, with a MIC of 0.3 μg/mL. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (312.11 mM), Sonication is recommended.
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| Keywords | membranes | Helicobacter | ulcer | Antimicrobial | gastric | inhibit | Inhibitor | Bacterial | permeate | HPi 1 | HPi-1 | orally | pylori | peptic | HPi1 |
| Inhibitors Related | Neomycin sulfate | Dehydroacetic acid sodium | Ampicillin sodium | Methyl anthranilate | Doxycycline (hyclate) | Kanamycin sulfate | G-418 disulfate | Sulfamethoxazole sodium | Metronidazole | Doxycycline | Dimethyl sulfoxide | Crystal Violet |
| Related Compound Libraries | Anti-Bacterial Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Anti-Infection Compound Library |
United States
