2. Anti-infection
  3. Bacterial
  4. HPi1

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.

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HPi1 Chemical Structure

HPi1 Chemical Structure

CAS No. : 13080-21-2

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HPi1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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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].

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HPi1 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

192.24

Formula

C8H8N4S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

S=C1NC2=C(C=CC=C2)N=C1NN
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (325.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (10.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

COA (248 KB) HNMR (238 KB) MS (79 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.2018 mL 26.0092 mL 52.0183 mL 130.0458 mL
5 mM 1.0404 mL 5.2018 mL 10.4037 mL 26.0092 mL
10 mM 0.5202 mL 2.6009 mL 5.2018 mL 13.0046 mL
15 mM 0.3468 mL 1.7339 mL 3.4679 mL 8.6697 mL
20 mM 0.2601 mL 1.3005 mL 2.6009 mL 6.5023 mL
25 mM 0.2081 mL 1.0404 mL 2.0807 mL 5.2018 mL
30 mM 0.1734 mL 0.8670 mL 1.7339 mL 4.3349 mL
40 mM 0.1300 mL 0.6502 mL 1.3005 mL 3.2511 mL
50 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6009 mL
60 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1674 mL
80 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6256 mL
100 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3005 mL
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HPi1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HPi113080-21-2HPi 1HPi-1BacterialAntimicrobialorallyHelicobacterpyloripepticulcergastricpermeatemembranesInhibitorinhibitorinhibit

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