| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
HPi1 targets Helicobacter pylori, a Gram-negative bacterium that colonizes the stomach and is a major cause of gastritis and peptic ulcers. Its selective antibacterial activity suggests it targets a specific pathway essential for H. pylori survival. It has some activity against Bacteroides species and Campylobacter jejuni, but at much higher concentrations.
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| ln Vitro |
The MIC range of H. pylori isolates in the agar dilution assay ranged from 0.01-0.17 μM, or 0.002-0.032 μg/mL. The strains ARHp172 (MIC 0.004–0.016 μg/mL) and ARHp246 (MIC 0.008–0.032 μg/mL) that are resistant to clarithromycin can be effectively inhibited by HPi1 [1]. Although HPi1 is at least eighteen times more concentrated than the minimum inhibitory concentration of Helicobacter pylori, it exhibits modest effect against Bacteroidetes. A MIC of 0.3 μg/mL was shown to indicate more powerful action for Campylobacter jejuni [1]. It has been observed that HPi1 possesses favorable physicochemical and pharmacological characteristics, such as determined water solubility (19 μg/mL), 93% binding to human plasma protein, human liver microsomal stability (T1/2 of 1.3 hours), and passively permeable membrane Ability[1].
In vitro, HPi1 is a highly potent and selective inhibitor of H. pylori, with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. It is effective against clarithromycin-resistant strains, with MICs ranging from 0.002 to 0.032 μg/mL in agar dilution assays. It shows minimal activity against other gut bacteria. |
| ln Vivo |
At doses of 25 or 50 mg/kg/day, treatment with HPi1 (6.25-50 mg/kg; oral gavage; once daily; for 3 days; female C57BL/6 mice) decreased colony counts below the detection limit [ 1].
In vivo, HPi1 is orally active, suggesting it can be administered by the oral route. Its activity against H. pylori in the gastrointestinal tract makes it a promising candidate for treating H. pylori infections. Further in vivo studies would be needed to confirm its efficacy and safety in animal models of infection. |
| Enzyme Assay |
In vitro antimicrobial assays for HPi1 involve determining its minimum inhibitory concentration (MIC) against H. pylori and other bacterial strains. Broth microdilution or agar dilution methods are used. The compound is tested against a panel of bacteria to assess its spectrum of activity and selectivity.
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| Cell Assay |
In vitro cell-based assays for HPi1 involve treating H. pylori cultures with the compound and measuring bacterial growth inhibition. The IC50 and MIC values are determined from dose-response curves. Its activity against clarithromycin-resistant strains is also assessed.
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| Animal Protocol |
Animal/Disease Models: Adult specific pathogen-free female C57BL/6 mice (6-8 weeks old), fed Helicobacter pylori SS1 suspension [1]
Doses: 6.25 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg Doses: po (oral gavage); one time/day; for 3 days. Experimental Results: The colony count diminished below the detection limit. In vivo animal experiments for HPi1 would involve infecting mice or other animal models with H. pylori and then treating them with the compound orally. Efficacy would be measured by bacterial clearance from the stomach and reduction in gastric inflammation. These studies have not been detailed in the search results. |
| ADME/Pharmacokinetics |
HPi1 has a molecular weight of 192.24 and a molecular formula of C8H8N4S. It has a melting point of 254°C (decomp.) and a density of 1.55±0.1 g/cm3. It is a solid with a light yellow to yellow appearance. It has good aqueous solubility (19 μg/mL).
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| Toxicity/Toxicokinetics |
HPi1 is a hazardous substance with a GHS08 warning symbol and a hazard statement H370 (causes damage to organs). It is for research use only and is not intended for human use. Standard safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
HPi1 is a potent, selective, and orally active antimicrobial agent against Helicobacter pylori. It has an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. It is inactive against other gut bacteria. It is effective against clarithromycin-resistant strains. HPi1 has good physicochemical properties, including aqueous solubility of 19 μg/mL, 93% human plasma protein binding, and a half-life of 1.3 hours in human liver microsomes.
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| Molecular Formula |
C8H8N4S
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| Molecular Weight |
192.24
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| Exact Mass |
192.047
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| CAS # |
13080-21-2
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| PubChem CID |
781248
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.55g/cm3
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| Boiling Point |
376.1ºC at 760 mmHg
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| Flash Point |
181.3ºC
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| Vapour Pressure |
7.41E-06mmHg at 25°C
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| Index of Refraction |
1.794
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| LogP |
1.977
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
251
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TVYAHCDRRICQJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H8N4S/c9-12-7-8(13)11-6-4-2-1-3-5(6)10-7/h1-4H,9H2,(H,10,12)(H,11,13)
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| Chemical Name |
3-hydrazinyl-1H-quinoxaline-2-thione
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| Synonyms |
HPi 1; HPi-1; HPi1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~325.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2018 mL | 26.0092 mL | 52.0183 mL | |
| 5 mM | 1.0404 mL | 5.2018 mL | 10.4037 mL | |
| 10 mM | 0.5202 mL | 2.6009 mL | 5.2018 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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