HPi1

Names

[ Name ]:
HPi1

[Synonym ]:
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

Biological Activity

[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]:

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[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]

[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.

Chemical & Physical Properties

[ 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

Safety Information

[ Hazard Codes ]:
Xn

[ HS Code ]:
2933990090

Customs

[ 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%

Related Compounds

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