3-HYDRAZINO-QUINOXALINE-2-THIOL
- CAS No.13080-21-2
- Chemical Name:3-HYDRAZINO-QUINOXALINE-2-THIOL
- CBNumber:CB1135666
- Molecular Formula:C8H8N4S
- Formula Weight:192.24
- MOL File:13080-21-2.mol
- Melting point 254 °C (decomp)(Solv: ethanol (64-17-5))
- Boiling point 376.1±25.0 °C(Predicted)
- Density 1.55±0.1 g/cm3(Predicted)
- pka 7.91±0.20(Predicted)
- form Solid
- color Light yellow to yellow
-
Symbol(GHS)
- Signal wordDanger
- Hazard statements H370
- Precautionary statements P501-P260-P270-P264-P308+P311-P405
3-HYDRAZINO-QUINOXALINE-2-THIOL Chemical Properties,Usage,Production
- Uses 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].
- Biological Activity HPi1 is a potent, selective and orally active antibacterial agent against Helicobacter pylori with IC50 of 0.24 μM and MIC of 0.08-0.16 μg/mL. It is inactive against other bacteria, including the enteric bacteria Lactobacillus casei, Lactobacillus reuteri and Bifidobacterium longum.
-
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 (T 1/2 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[1].
Animal Model: Adult specific-pathogen-free female C57BL/6 mice (6-8-week-old) fed with H. pylori SS1 suspension[1] 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. -
target
IC50: 0.24 μM ( Helicobacter pylori )
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MIC: 0.08-0.16 μg/mL ( Helicobacter pylori )- References [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. DOI:10.1128/AAC.02573-13
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