| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ADAM17 (a disintegrin and metalloproteinase 17) and MMP-12 (matrix metalloproteinase-12) with IC₅₀ of 9.4 nM. JG26 inhibits AngII-induced EGFR transactivation and ERK activation in vascular smooth muscle cells.
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|---|---|
| ln Vitro |
JG26 inhibits MMP-12 with an IC₅₀ of 9.4 nM. It suppresses AngII-induced EGFR transactivation and ERK activation in cultured VSMCs. JG26 increases ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. The compound has shown promising results in combating viral infections, particularly coronaviruses.
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| ln Vivo |
JG26 has shown promising results in combating viral infections, particularly those caused by coronaviruses. It reduces SARS-CoV-2 infection. JG26 suppresses AngII-induced EGFR transactivation and ERK activation in vivo. Detailed in vivo efficacy in animal models of viral infection has been reported.
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| Enzyme Assay |
ADAM17 enzymatic activity assay: Recombinant ADAM17 is incubated with varying concentrations of JG26 and a fluorogenic peptide substrate in assay buffer at 37°C for 30-60 min. The cleavage of the substrate is measured by fluorescence. IC₅₀ values are calculated. MMP-12 activity assay: Recombinant MMP-12 is incubated with JG26 and a fluorogenic substrate; IC₅₀ is calculated.
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| Cell Assay |
EGFR transactivation assay: Vascular smooth muscle cells are treated with JG26 at varying concentrations and stimulated with AngII. EGFR phosphorylation is measured by Western blot using anti-phospho-EGFR antibody. ERK activation is assessed by anti-phospho-ERK Western blot. ACE2 expression is measured by Western blot or qPCR.
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| Animal Protocol |
SARS-CoV-2 infection model: Cells are treated with JG26 prior to SARS-CoV-2 infection. Viral load is measured by qRT-PCR for viral RNA. The reduction in infection is assessed compared to vehicle-treated controls. In vivo models would involve infected animals with JG26 administration and viral load measurement.
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| ADME/Pharmacokinetics |
JG26 has a CAS number of 1464910-32-4. It is an ADAM17 inhibitor with additional MMP-12 inhibitory activity (IC₅₀ = 9.4 nM). Comprehensive PK parameters such as bioavailability and half-life remain to be characterized. The compound is for research use only.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published. JG26 is for research use only. Standard laboratory safety practices should be followed when handling this compound. As a metalloproteinase inhibitor, potential effects on ECM remodeling and immune function should be considered.
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| References | |
| Additional Infomation |
JG26 is an ADAM17 inhibitor that also inhibits MMP-12 with an IC₅₀ of 9.4 nM. It suppresses AngII-induced EGFR transactivation and ERK activation. JG26 upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. The compound has antiviral potential. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C19H22BR2N4O6S
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|---|---|
| Molecular Weight |
594.274181842804
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| Exact Mass |
591.962
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| CAS # |
1464910-32-4
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| PubChem CID |
72714324
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
32
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| Complexity |
705
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(NO)(=O)[C@H](NS(C1=CC=C(OCC2=CC(Br)=CC(Br)=C2)C=C1)(=O)=O)CCCNC(N)=O
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| InChi Key |
QTXVPJOTKLUYMQ-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C19H22Br2N4O6S/c20-13-8-12(9-14(21)10-13)11-31-15-3-5-16(6-4-15)32(29,30)25-17(18(26)24-28)2-1-7-23-19(22)27/h3-6,8-10,17,25,28H,1-2,7,11H2,(H,24,26)(H3,22,23,27)/t17-/m1/s1
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| Chemical Name |
(2R)-5-(carbamoylamino)-2-[[4-[(3,5-dibromophenyl)methoxy]phenyl]sulfonylamino]-N-hydroxypentanamide
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| Synonyms |
JG-26; JG 26; JG26
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~168.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.21 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 25.0 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: ≥ 2.5 mg/mL (4.21 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 25.0 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: ≥ 2.5 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6827 mL | 8.4137 mL | 16.8274 mL | |
| 5 mM | 0.3365 mL | 1.6827 mL | 3.3655 mL | |
| 10 mM | 0.1683 mL | 0.8414 mL | 1.6827 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.