HPi1

SKU: orb1218947

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.

Key Properties

• CAS Number: 13080-21-2
• MW: 192.24
• Purity: >98% (HPLC)
• Formula: C₈H₈N₄S
• SMILES: S=C1NC2=C(C=CC=C2)N=C1NN
• Target: Helicobacter pylori
• Solubility: DMSO : 60 mg/mL (312.11 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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. Animal model: Adult specific-pathogen-free female C57BL/6 mice (6-8-week-old) fed with H. pylori SS1 suspension. Dosage: 6.25 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg. Administration: Oral gavage; once a day; for 3 days. Result: Reduced colony counts to below the limit of detection.
• In Vitro:
  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). 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Helicobacter pylori