| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
The primary target of pGlu-Pro-Arg-MNA monoacetate is protein C, a serine protease that is activated by the thrombin-thrombomodulin complex on the endothelial cell surface. Activated protein C (APC) functions as an anticoagulant by proteolytically inactivating coagulation factors Va and VIIIa. The peptide substrate contains the sequence Pro-Arg, which is recognized and cleaved by activated protein C. Upon cleavage, the chromogenic or fluorogenic leaving group (MNA, 4-methoxy-2-naphthylamine) is released, producing a detectable signal. This substrate is used to measure protein C activity in plasma and other biological samples.
|
|---|---|
| ln Vitro |
Using reagents such as a chromogenic substrate (pGlu-Pro-Arg-mNA) and a partial thromboplastin time (aPTT) system, protein C activity is determined by photometric analysis [1].
In vitro studies of pGlu-Pro-Arg-MNA monoacetate focus on its use as a substrate for measuring protein C activity. The peptide is incubated with samples containing protein C (such as plasma), and the cleavage of the substrate releases a chromogenic or fluorogenic product that can be quantified spectrophotometrically or fluorometrically. The rate of substrate cleavage is proportional to protein C activity. This assay is used to measure protein C activity in purified systems, plasma, and other biological samples. The substrate is also used to study the regulation of protein C activation and to screen for modulators of protein C activity. pGlu-Pro-Arg-MNA monoacetate is a widely used substrate for protein C assays. |
| ln Vivo |
In vivo studies of pGlu-Pro-Arg-MNA monoacetate are not typically performed, as the compound is used as an in vitro diagnostic reagent rather than a therapeutic agent. However, the substrate could be used in ex vivo assays to measure protein C activity in plasma samples from animal models of thrombosis or hemostasis. By measuring protein C activity, the substrate can help evaluate the effects of anticoagulant drugs or disease states on the protein C pathway. The compound's utility in such applications depends on its stability and specificity for protein C. It is primarily a research tool for studying protein C biology and the regulation of blood coagulation.
|
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, pGlu-Pro-Arg-MNA monoacetate is used as a chromogenic or fluorogenic substrate in protein C activity assays. The substrate is incubated with activated protein C or samples containing protein C (such as plasma) at physiological pH and temperature. The cleavage of the substrate releases a chromogenic or fluorogenic product (MNA, 4-methoxy-2-naphthylamine) that can be quantified by measuring fluorescence or absorbance. The rate of fluorescence or absorbance increase is proportional to protein C activity. Kinetic parameters such as Kₘ and Vₘₐₓ can be determined. Inhibitors or activators of protein C can be evaluated by measuring changes in protein C activity in the presence of the test compound.
|
| Cell Assay |
For in vitro cellular experiments, pGlu-Pro-Arg-MNA monoacetate is not typically used in cell-based assays, as it is a substrate for protein C rather than a modulator of cellular function. However, the substrate can be used in assays measuring protein C activity in cell culture supernatants or in cell-based models of coagulation. For example, protein C activity can be measured in the conditioned media of endothelial cells or other cells that produce protein C. The substrate can also be used to measure the activity of protein C generated in plasma samples. These assays are useful for studying the regulation of protein C activation and activity in cellular and physiological contexts.
|
| Animal Protocol |
For in vivo animal experiments, pGlu-Pro-Arg-MNA monoacetate is not typically administered to animals, as it is used as an in vitro reagent. However, blood samples from animals can be collected and the substrate can be used ex vivo to measure protein C activity in plasma. This approach can be used to evaluate the effects of drug treatments or disease states on protein C activity in animal models. For example, protein C activity can be measured in plasma from animals treated with anticoagulants or in models of thrombosis. The substrate provides a sensitive and specific method for quantifying protein C activity in biological samples.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of pGlu-Pro-Arg-MNA monoacetate are not relevant, as the compound is used as an in vitro reagent rather than a therapeutic agent. The peptide is not administered to animals or humans for therapeutic purposes. Its stability in solution and under assay conditions is important for its use as a research reagent. The compound should be stored appropriately to maintain its activity and stability. As a peptide substrate, it is susceptible to degradation by proteases, and care should be taken to avoid contamination. The compound is typically stored as a dry powder at -20degC.
|
| Toxicity/Toxicokinetics |
Toxicological data for pGlu-Pro-Arg-MNA monoacetate are limited, as it is used as a research reagent rather than a therapeutic agent. The compound is generally considered to have low toxicity for in vitro use. However, as with all research chemicals, appropriate safety precautions should be taken when handling the compound, including the use of personal protective equipment and adherence to institutional safety guidelines. The fluorogenic leaving group (MNA, 4-methoxy-2-naphthylamine) may have its own toxicity profile, but the amounts used in assays are typically very small. The compound should be handled with care to avoid inhalation, ingestion, or skin contact.
|
| References |
[1]. Girolami A, et al. Heterozygous protein-S deficiency: a study of a large kindred. Acta Haematol. 1990;84(3):162-8.
|
| Additional Infomation |
pGlu-Pro-Arg-MNA monoacetate is a chromogenic/fluorogenic peptide substrate used for measuring protein C activity in vitro. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The substrate is widely employed in protease activity assays, especially for measuring protein C activity. It is used with partial thromboplastin time (aPTT) reagents for the photometric determination of protein C activity. pGlu-Pro-Arg-MNA monoacetate is a valuable tool for studying the protein C pathway and for diagnosing protein C deficiency.
|
| Molecular Formula |
C25H36N8O9
|
|---|---|
| Molecular Weight |
592.601545333862
|
| Exact Mass |
592.26
|
| CAS # |
2070009-26-4
|
| Related CAS # |
pGlu-Pro-Arg-MNA;130835-45-9
|
| PubChem CID |
138115114
|
| Appearance |
Off-white to light yellow solid powder
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
42
|
| Complexity |
966
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=O)O.COC1=C(C=CC(=C1)[N+](=O)[O-])NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]3CCC(=O)N3
|
| InChi Key |
NPFQYEIMISHQDL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H32N8O7.C2H4O2/c1-38-18-12-13(31(36)37)6-7-14(18)28-20(33)15(4-2-10-26-23(24)25)29-21(34)17-5-3-11-30(17)22(35)16-8-9-19(32)27-16;1-2(3)4/h6-7,12,15-17H,2-5,8-11H2,1H3,(H,27,32)(H,28,33)(H,29,34)(H4,24,25,26);1H3,(H,3,4)
|
| Chemical Name |
acetic acid;N-[5-(diaminomethylideneamino)-1-(2-methoxy-4-nitroanilino)-1-oxopentan-2-yl]-1-(5-oxopyrrolidine-2-carbonyl)pyrrolidine-2-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ≥ 25 mg/mL (~42.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6875 mL | 8.4374 mL | 16.8748 mL | |
| 5 mM | 0.3375 mL | 1.6875 mL | 3.3750 mL | |
| 10 mM | 0.1687 mL | 0.8437 mL | 1.6875 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
