| Identification | Back Directory | [Name]
3-HYDRAZINO-QUINOXALINE-2-THIOL | [CAS]
13080-21-2 | [Synonyms]
AKOS BBS-00008251
CHEMBRDG-BB 5215319
3-HYDRAZINO-QUINOXALINE-2-THIOL
3-Hydrazinylquinoxaline-2-thiol
2(1H)-Quinoxalinethione, 3-hydrazinyl-
3-hydrazinoquinoxaline-2-thiol(SALTDATA: FREE) | [Molecular Formula]
C8H8N4S | [MDL Number]
MFCD00457014 | [MOL File]
13080-21-2.mol | [Molecular Weight]
192.24 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
7.91±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [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 )
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 |
|
| Company Name: |
Alfa Chemistry
|
| Tel: |
1-516-6625404 |
| Website: |
https://www.alfa-chemistry.com |
|