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| 25mg |
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| Targets |
HZ-1157 targets the HCV NS3/4A protease, a key enzyme in the viral replication complex responsible for the cleavage of the viral polyprotein. By inhibiting this protease, it prevents the production of mature viral proteins and thereby inhibits viral replication. The compound has also been reported to inhibit plasma kallikrein, reducing the generation of bradykinin, a mediator of inflammation, pain, and vascular permeability. Additionally, it inhibits dihydrofolate reductase (DHFR).
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| ln Vitro |
Numerous biological actions of HZ-1157 (4a) are known to exist, including dihydrofolate reductase inhibition, SMN2 promoter activation, and inhibition of protein lysine methyltransferase G9a[1][2].
HZ-1157 demonstrates potent inhibition of HCV NS3/4A protease with an IC50 of 1.0 μmol/L. It exhibits high activity against dengue virus with an EC50 of 0.15 μM. The compound has a CC50 > 10 μM, indicating relatively low cytotoxicity. It also inhibits protein lysine methyltransferase G9a, activates the SMN2 promoter, and inhibits dihydrofolate reductase. |
| ln Vivo |
HZ-1157 has shown efficacy in inhibiting HCV replication in cell-based assays. Its broad-spectrum antiviral activity against dengue virus has also been confirmed in vitro. The compound's activity against plasma kallikrein suggests potential therapeutic applications in conditions involving bradykinin-mediated inflammation, such as hereditary angioedema. However, detailed in vivo efficacy data in animal models is limited.
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| Enzyme Assay |
The primary in vitro assay for HZ-1157 is a protease inhibition assay using purified HCV NS3/4A protease. The enzyme is incubated with a fluorogenic peptide substrate, and the cleavage of the substrate is measured in the presence of the compound. The IC50 of 1.0 μmol/L is determined from dose-response curves. DHFR inhibition can be assessed using a standard dihydrofolate reductase assay.
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| Cell Assay |
Cell viability assay [2].
Cell Types: HZ-1157 (4a) is known to have a wide range of biological activities, such as protein lysine methyltransferase G9a inhibition, SMN2 promoter activation, dihydrofolate reductase inhibition, etc. Tested Concentrations: 0-10μmol/L. Incubation Duration: 72 hrs (hours). Experimental Results: Inhibited HCV infection in vitro, IC50 was 0.82 μmol/L. In vitro cellular experiments for HZ-1157 involve treating HCV replicon cells or dengue virus-infected cells with the compound. Viral replication is measured by quantifying viral RNA levels using real-time PCR or by measuring the expression of reporter genes. The CC50 is determined using standard cell viability assays such as MTT or CellTiter-Glo. |
| Animal Protocol |
In vivo animal experiments for HZ-1157 are not extensively detailed in the available literature. As an antiviral agent, it could be evaluated in animal models of HCV or dengue virus infection to assess its efficacy in reducing viral load. Its effects on bradykinin-mediated inflammation could be assessed in models of hereditary angioedema or inflammatory diseases.
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| ADME/Pharmacokinetics |
HZ-1157 has a molecular weight of approximately 248.28 g/mol and a molecular formula of C12H16N4O. It is a small molecule that is typically used as a research reagent. It is soluble in DMSO. Its purity is typically ≥98%. The compound is stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
HZ-1157 is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. It has been reported to have relatively low cytotoxicity (CC50 > 10 μM). As with all research chemicals, standard safety precautions should be followed when handling.
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| References | |
| Additional Infomation |
Antiviral agent; structure as described in the first source.
HZ-1157 is a potent inhibitor of the HCV NS3/4A protease with an IC50 of 1.0 μmol/L. It exhibits broad-spectrum antiviral activity, including high activity against dengue virus (EC50 = 0.15 μM). HZ-1157 also inhibits protein lysine methyltransferase G9a, activates the SMN2 promoter, and inhibits dihydrofolate reductase. It is being explored for therapeutic applications in viral infections and inflammatory diseases. |
| Molecular Formula |
C12H16N4O
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|---|---|
| Molecular Weight |
232.287
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| Exact Mass |
232.132
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| Elemental Analysis |
C, 62.05; H, 6.94; N, 24.12; O, 6.89
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| CAS # |
1009734-33-1
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| PubChem CID |
24778294
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
471.6±53.0 °C at 760 mmHg
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| Flash Point |
239.0±30.9 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
266
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1=CC=CC2C1=C(N)N=C(N)N=2)C(C)(C)C
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| InChi Key |
JQHKDYFLRJIBLX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H16N4O/c1-12(2,3)17-8-6-4-5-7-9(8)10(13)16-11(14)15-7/h4-6H,1-3H3,(H4,13,14,15,16)
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| Chemical Name |
5-(1,1-Dimethylethoxy)- 2,4-quinazolinediamine
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| Synonyms |
HZ-1157; HZ 1157; HZ1157. Dengue Virus Inhibitor II.
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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 : ~20 mg/mL (~86.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (8.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (8.61 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 20.0 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. View More
Solubility in Formulation 3: ≥ 2 mg/mL (8.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2 mg/mL (8.61 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3050 mL | 21.5248 mL | 43.0496 mL | |
| 5 mM | 0.8610 mL | 4.3050 mL | 8.6099 mL | |
| 10 mM | 0.4305 mL | 2.1525 mL | 4.3050 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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