| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Suc-AAPF-pNA is a substrate for serine proteases, including cathepsin G, chymotrypsin, chymase, subtilisins, and cyclophilin. It is not cleaved by neutrophil elastase. The substrate contains the amino acid sequence Ala-Ala-Pro-Phe, which is recognized and cleaved by these proteases at the Phe-pNA bond. The release of p-nitroaniline allows for spectrophotometric quantification of enzyme activity. This substrate is used to study enzyme kinetics and protease activity in biological samples.
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|---|---|
| ln Vitro |
Suc-AAPF-pNA is cleaved by cathepsin G with a Km of 1.7 mM. It is also cleaved by chymotrypsin (Km = 60 µM), chymase (Km = 4 mM), subtilisins, and cyclophilin, but not by neutrophil elastase. The cleavage releases 4-nitroaniline, which is yellow and can be measured at 405-410 nm. The substrate is used to measure free and membrane-bound cathepsin G activity in human neutrophils.
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| ln Vivo |
Suc-AAPF-pNA is not a therapeutic agent and does not have in vivo activity in the traditional sense. It is used as a research tool to measure protease activity in biological samples. Its utility lies in its ability to report on the activity of specific proteases in vitro and ex vivo. No in vivo pharmacological activity is associated with this substrate.
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| Enzyme Assay |
The non-cellular enzyme assay for Suc-AAPF-pNA involves incubating the substrate with purified enzyme (e.g., cathepsin G, chymotrypsin, or chymase) in assay buffer. The reaction is monitored spectrophotometrically at 405-410 nm to measure the release of p-nitroaniline. Initial reaction rates are calculated from the linear portion of the absorbance vs. time curve. Km and Vmax values are determined from Michaelis-Menten kinetics using varying substrate concentrations. Enzyme inhibitors can be evaluated by measuring the decrease in reaction rate.
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| Cell Assay |
In vitro cellular assays for Suc-AAPF-pNA typically involve the measurement of cathepsin G activity in cell lysates or on the surface of human neutrophils. Cells are lysed or intact cells are incubated with the substrate in appropriate buffer. The release of p-nitroaniline is measured spectrophotometrically at 405-410 nm. Activity can be measured in the presence or absence of protease inhibitors to confirm specificity. This assay is used to study cathepsin G activity in inflammatory and immune cells.
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| Animal Protocol |
In vivo animal studies for Suc-AAPF-pNA are not conducted, as the compound is a research substrate rather than a therapeutic agent. It is used ex vivo to measure protease activity in biological samples collected from animal models. No in vivo administration of this substrate is performed for pharmacological evaluation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Suc-AAPF-pNA are not relevant, as the compound is not a therapeutic agent and is not administered in vivo. It is used exclusively as a research tool in in vitro and ex vivo assays. Any PK properties would be irrelevant to its intended use.
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| Toxicity/Toxicokinetics |
Toxicological data for Suc-AAPF-pNA are limited. As a research-grade peptide substrate, it is generally considered to have low toxicity. The compound may cause skin and eye irritation upon contact. Standard laboratory safety precautions should be observed when handling this compound. It is not intended for human or animal consumption.
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| Additional Infomation |
Suc-AAPF-pNA is a research-grade chromogenic substrate intended for laboratory use only. It is not approved for clinical use as a therapeutic agent. Its primary applications include measuring cathepsin G activity in human neutrophils, studying the enzymatic kinetics of serine proteases, and screening for protease inhibitors. The compound is also known as N-Succinyl-Ala-Ala-Pro-Phe-pNA and is widely used in enzymology and protease research.
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| Molecular Formula |
C30H36N6O9
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|---|---|
| Molecular Weight |
624.64200
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| Exact Mass |
624.254
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| CAS # |
70967-97-4
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| PubChem CID |
5496888
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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 |
1072.8±65.0 °C at 760 mmHg
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| Flash Point |
602.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.614
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| LogP |
2.58
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
45
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| Complexity |
1100
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| Defined Atom Stereocenter Count |
4
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| SMILES |
N1(CCC[C@H]1C(=O)N[C@H](C(=O)NC1=CC=C([N+]([O-])=O)C=C1)CC1=CC=CC=C1)C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)CCC(=O)O
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| InChi Key |
LKDMKWNDBAVNQZ-WJNSRDFLSA-N
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| InChi Code |
InChI=1S/C30H36N6O9/c1-18(31-25(37)14-15-26(38)39)27(40)32-19(2)30(43)35-16-6-9-24(35)29(42)34-23(17-20-7-4-3-5-8-20)28(41)33-21-10-12-22(13-11-21)36(44)45/h3-5,7-8,10-13,18-19,23-24H,6,9,14-17H2,1-2H3,(H,31,37)(H,32,40)(H,33,41)(H,34,42)(H,38,39)/t18-,19-,23-,24-/m0/s1
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| Chemical Name |
4-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-(4-nitroanilino)-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-oxobutanoic 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 : ~100 mg/mL (~160.09 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.00 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 (4.00 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 (4.00 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 | 1.6009 mL | 8.0046 mL | 16.0092 mL | |
| 5 mM | 0.3202 mL | 1.6009 mL | 3.2018 mL | |
| 10 mM | 0.1601 mL | 0.8005 mL | 1.6009 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.