| Name | 3-hydrazinyl-1H-quinoxaline-2-thione |
|---|---|
| Synonyms |
2-mercapto-3-hydrazinoquinoxaline
3-hydrazinylquinoxaline-2-thiol 3-hydrazino-1H-quinoxaline-2-thione 3-hydrazinoquinoxaline-2-thiol 3-Hydrazino-1H-chinoxalin-2-thion 3-hydrazinylquinoxaline-2(1H)-thione 3-hydrazinoquinoxaline-2-thione |
| 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[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.24 μM (Helicobacter pylori)[1] MIC: 0.08-0.16 μg/mL (Helicobacter pylori)[1] |
| 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)[1]. 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[1]. 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[1]. |
| 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. |
| References |
| Density | 1.55g/cm3 |
|---|---|
| Boiling Point | 376.1ºC at 760 mmHg |
| Molecular Formula | C8H8N4S |
| Molecular Weight | 192.24100 |
| Flash Point | 181.3ºC |
| Exact Mass | 192.04700 |
| PSA | 102.63000 |
| LogP | 1.97740 |
| Vapour Pressure | 7.41E-06mmHg at 25°C |
| Index of Refraction | 1.794 |
| Hazard Codes | Xn |
|---|---|
| HS Code | 2933990090 |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |