Description
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.
Product information
CAS Number: 13080-21-2
Molecular Weight: 463.52
Formula: C27H29NO6
Chemical Name: 2-methoxyethyl 4-(3-hydroxyphenyl)-7-(2-methoxyphenyl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
Smiles: CC1NC2CC(CC(=O)C=2C(C=1C(=O)OCCOC)C1=CC(O)=CC=C1)C1=CC=CC=C1OC
InChiKey: ZXSWZQSYZYMZKS-UHFFFAOYSA-N
InChi: InChI=1S/C27H29NO6/c1-16-24(27(31)34-12-11-32-2)25(17-7-6-8-19(29)13-17)26-21(28-16)14-18(15-22(26)30)20-9-4-5-10-23(20)33-3/h4-10,13,18,25,28-29H,11-12,14-15H2,1-3H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (325.11 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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