| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
The primary molecular target of Z-Gly-Gly-Arg-AMC acetate is thrombin, a key serine protease that regulates the blood coagulation cascade. The compound is a thrombin-specific fluorogenic substrate that is cleaved by thrombin at the Arg-AMC bond. Upon cleavage, the AMC fluorophore is released, generating a fluorescent signal that can be measured. The substrate is used to detect thrombin production in platelet-rich plasma (PRP) and platelet-poor plasma (PPP). It is also a substrate for other serine proteases, including urokinase, tissue-type plasminogen activator, and trypsin.
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| ln Vitro |
In vitro, Z-Gly-Gly-Arg-AMC acetate is used as a fluorogenic substrate to measure the activity of thrombin and other serine proteases. The substrate is cleaved by the target protease, releasing the AMC fluorophore, which can be detected by fluorescence spectroscopy with excitation at 390 nm and emission at 480 nm. The increase in fluorescence over time is proportional to the enzyme activity. The compound is used in assays to test thrombin generation in PRP and PPP. It is also used for a direct fluorometric assay of urokinase, tissue-type plasminogen activator, trypsin, and thrombin. The substrate's specificity for thrombin makes it a valuable tool for studying coagulation and thrombosis.
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| ln Vivo |
In vivo studies of Z-Gly-Gly-Arg-AMC acetate are limited, as the compound is primarily used as a research reagent for in vitro assays rather than as a therapeutic agent. The substrate is used to measure thrombin generation in plasma samples, which can provide information about the coagulation status of patients. However, the compound itself is not administered in vivo. No extensive in vivo pharmacological or toxicological studies have been reported for this substrate. The compound is used for research purposes only and is not intended for therapeutic use.
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| Enzyme Assay |
For thrombin activity assays, Z-Gly-Gly-Arg-AMC acetate is dissolved in an appropriate buffer (e.g., 50 mM Tris-HCl, pH 7.4, containing 150 mM NaCl and 0.1% BSA). The substrate is typically used at concentrations ranging from 10 to 100 µM. Thrombin or plasma samples are added to the substrate solution in a 96-well plate. The reaction is incubated at 37°C for a specified time, and fluorescence is measured continuously or at endpoint using a fluorescence plate reader with excitation at 390 nm and emission at 480 nm. The increase in fluorescence is proportional to thrombin activity. For kinetic studies, initial reaction rates are calculated, and Km and Vmax values are determined from Michaelis-Menten plots.
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| Cell Assay |
For cellular studies, Z-Gly-Gly-Arg-AMC acetate is typically not used in cell-based assays, as it is a substrate for enzymatic assays in plasma or purified enzyme systems. However, the compound may be used to measure thrombin activity in cell culture supernatants or cell lysates. Cells are cultured and stimulated to produce thrombin or other proteases. The supernatant or lysate is collected and incubated with the substrate. Fluorescence is measured as described above. The substrate can also be used to assess the activity of thrombin in the presence of test compounds to evaluate their inhibitory effects.
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| Animal Protocol |
Standard in vivo protocols for Z-Gly-Gly-Arg-AMC acetate are not applicable, as the compound is used as an in vitro research reagent. It is not administered to animals. The compound is used to measure thrombin generation in plasma samples collected from animals or humans in ex vivo assays. No specific in vivo protocols are reported in the literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Z-Gly-Gly-Arg-AMC acetate are not applicable, as the compound is used as an in vitro research reagent and is not intended for in vivo use. The compound is not administered systemically, and no ADME studies have been reported. It is used as a substrate in enzymatic assays and is not designed for therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicological data for Z-Gly-Gly-Arg-AMC acetate are limited, as the compound is used as a research reagent. The compound is generally considered to have low toxicity at the concentrations used for enzymatic assays (typically 10-100 µM). No acute toxicity, mutagenicity, or carcinogenicity data have been reported. As with all chemical reagents, appropriate safety precautions should be taken when handling Z-Gly-Gly-Arg-AMC acetate, including the use of personal protective equipment and work in a well-ventilated area.
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| References |
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| Additional Infomation |
Z-Gly-Gly-Arg-AMC acetate (CAS 2070009-61-7) is a thrombin-specific fluorogenic substrate for testing thrombin generation in PRP and PPP. It consists of a Z-Gly-Gly-Arg peptide sequence linked to an AMC fluorophore. The compound has a molecular formula of C₃₀H₃₇N₇O₉ and a molecular weight of 639.66. It exhibits excitation/emission at 390/480 nm. The substrate is cleaved by thrombin, releasing AMC and generating a fluorescent signal. It is also used for assays of urokinase, tissue-type plasminogen activator, and trypsin. The compound is strictly for research use only.
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| Molecular Formula |
C30H37N7O9
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| Molecular Weight |
639.65628695488
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| Exact Mass |
639.265
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| CAS # |
2070009-61-7
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| Related CAS # |
Z-Gly-Gly-Arg-AMC;66216-78-2
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| PubChem CID |
92044473
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
46
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(=O)(O)C.CC1=CC(=O)OC2=CC(NC(=O)[C@H](CCCNC(N)=N)NC(=O)CNC(=O)CNC(=O)OCC3C=CC=CC=3)=CC=C12
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| InChi Key |
AVVGJZBMODPHEX-BOXHHOBZSA-N
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| InChi Code |
InChI=1S/C28H33N7O7.C2H4O2/c1-17-12-25(38)42-22-13-19(9-10-20(17)22)34-26(39)21(8-5-11-31-27(29)30)35-24(37)15-32-23(36)14-33-28(40)41-16-18-6-3-2-4-7-18;1-2(3)4/h2-4,6-7,9-10,12-13,21H,5,8,11,14-16H2,1H3,(H,32,36)(H,33,40)(H,34,39)(H,35,37)(H4,29,30,31);1H3,(H,3,4)/t21-;/m0./s1
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| Chemical Name |
acetic acid;benzyl N-[2-[[2-[[(2S)-5-(diaminomethylideneamino)-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamate
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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 (~156.33 mM)
H2O : ~20 mg/mL (~31.27 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (6.52 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 41.7 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: ≥ 4.17 mg/mL (6.52 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 41.7 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: ≥ 4.17 mg/mL (6.52 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 | 1.5633 mL | 7.8167 mL | 15.6333 mL | |
| 5 mM | 0.3127 mL | 1.5633 mL | 3.1267 mL | |
| 10 mM | 0.1563 mL | 0.7817 mL | 1.5633 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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