| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cathepsin G
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|---|---|
| ln Vitro |
Cathepsin G Inhibitor I exhibits reversible and competitive inhibition of Cathepsin G with an IC50 of 53 nM and a Ki of 63 nM. It shows high selectivity, weakly inhibiting chymotrypsin (Ki = 1.5 uM) and showing no significant inhibition of thrombin, Factor Xa, plasmin, trypsin, or elastase (IC50 >100 uM).
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| ln Vivo |
Currently, no specific in vivo data is available for this compound. General in vivo information for similar selective protease inhibitors may include their ability to reduce inflammation, modulate immune cell recruitment, and prevent tissue damage in animal models of arthritis or asthma.
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| Enzyme Assay |
A typical serine protease inhibition assay uses a chromogenic substrate like Suc-Ala-Ala-Pro-Phe-pNA for Cathepsin G. The compound is pre-incubated with the enzyme in a buffer (e.g., 50 mM Tris-HCl, pH 7.5, 150 mM NaCl) at 25degC for 5 minutes. The reaction is initiated by adding the substrate, and absorbance at 405 nm is monitored to calculate IC50 and Ki.
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| Cell Assay |
A general cellular protocol for studying cathepsin G involves using human neutrophils or U937 cells differentiated into neutrophil-like cells. Cells are pre-incubated with the inhibitor, then stimulated with a compound like fMLP or PMA. The activity of secreted cathepsin G is measured in the cell supernatant using a specific substrate, or the inhibitor's effect on T cell responses is assessed.
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| Animal Protocol |
General in vivo procedures for studying cathepsin G inhibitors involve using a mouse model of LPS-induced lung inflammation. The compound is administered via intratracheal or intraperitoneal injection 1 hour prior to LPS challenge. Bronchoalveolar lavage fluid is collected to measure neutrophil influx, elastase activity, and pro-inflammatory cytokine levels (e.g., IL-6, TNF-alpha).
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| ADME/Pharmacokinetics |
Cathepsin G Inhibitor I has a molecular weight of 620.63. As a non-peptide inhibitor, it may have better metabolic stability than peptide-based inhibitors. It is soluble in DMSO and is typically administered via injection in in vivo studies due to potential solubility limitations for oral dosing.
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| Toxicity/Toxicokinetics |
Cathepsin G Inhibitor I is considered a research tool with low reported toxicity. No specific LD50 or detailed safety data is available, but handling should follow standard laboratory safety practices for chemical reagents. It is not intended for human use and no clinical toxicity data exists.
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| References | |
| Additional Infomation |
Cathepsin G Inhibitor I is a high-quality research tool used extensively to dissect the biological functions of Cathepsin G. It is used in antigen-processing studies and for modulation of T cell responses in situ and in vivo. It is also a valuable reference compound for developing new therapeutic candidates targeting serine proteases.
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| Molecular Formula |
C36H33N2O6P
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|---|---|
| Molecular Weight |
620.63
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| Exact Mass |
620.207
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| CAS # |
429676-93-7
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| PubChem CID |
9830518
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
912.0±75.0 °C at 760 mmHg
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| Flash Point |
505.4±37.1 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.713
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| LogP |
2.01
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
45
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C1CCN(CC1)C(=O)C2=CC=CC=C2)C(=O)C3=CC4=CC=CC=C4C=C3C(=O)C(C5=CC=CC6=CC=CC=C65)P(=O)(O)O
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| InChi Key |
GNOZQRKYZJSIPZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H33N2O6P/c1-37(28-18-20-38(21-19-28)35(40)25-11-3-2-4-12-25)36(41)32-23-27-14-6-5-13-26(27)22-31(32)33(39)34(45(42,43)44)30-17-9-15-24-10-7-8-16-29(24)30/h2-17,22-23,28,34H,18-21H2,1H3,(H2,42,43,44)
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| Chemical Name |
[2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 10 mg/mL (16.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.03 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 (4.03 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 (4.03 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 | 1.6113 mL | 8.0563 mL | 16.1127 mL | |
| 5 mM | 0.3223 mL | 1.6113 mL | 3.2225 mL | |
| 10 mM | 0.1611 mL | 0.8056 mL | 1.6113 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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