| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
The primary target of Tos-Gly-Pro-Arg-ANBA-IPA acetate is thrombin, a serine protease that plays a central role in the coagulation cascade. Thrombin converts fibrinogen to fibrin, activates platelets, and amplifies its own generation through feedback activation of coagulation factors. The peptide substrate contains the sequence Gly-Pro-Arg, which is recognized and cleaved by thrombin. Upon cleavage, the chromogenic or fluorogenic leaving group (ANBA-IPA) is released, producing a detectable signal. This substrate is used to measure thrombin activity in vitro, enabling the study of thrombin function and the screening of thrombin inhibitors.
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| ln Vitro |
In vitro studies of Tos-Gly-Pro-Arg-ANBA-IPA acetate focus on its use as a substrate for measuring thrombin activity. The peptide is incubated with thrombin or thrombin-containing samples (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 thrombin activity. This assay is used to measure thrombin activity in purified systems, plasma, and other biological samples. The substrate is also used to screen for thrombin inhibitors and to study the kinetics of thrombin-catalyzed reactions. Tos-Gly-Pro-Arg-ANBA-IPA acetate is a highly specific substrate for thrombin.
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| ln Vivo |
In vivo studies of Tos-Gly-Pro-Arg-ANBA-IPA acetate 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 thrombin activity in plasma samples from animal models of thrombosis or hemostasis. By measuring thrombin activity, the substrate can help evaluate the effects of anticoagulant drugs or disease states on the coagulation system. The compound's utility in such applications depends on its stability and specificity for thrombin. It is primarily a research tool for studying thrombin biology and coagulation.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, Tos-Gly-Pro-Arg-ANBA-IPA acetate is used as a chromogenic substrate in thrombin activity assays. The substrate is incubated with purified thrombin or thrombin-containing samples at physiological pH and temperature. The cleavage of the substrate releases a chromogenic product (typically p-nitroaniline or a related chromophore) that can be quantified by measuring absorbance at a specific wavelength (e.g., 405 nm). The rate of absorbance increase is proportional to thrombin activity. Kinetic parameters such as Kₘ and Vₘₐₓ can be determined by measuring the initial rate of substrate cleavage at various substrate concentrations. Inhibitors can be evaluated by measuring the reduction in thrombin activity in the presence of the inhibitor.
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| Cell Assay |
For in vitro cellular experiments, Tos-Gly-Pro-Arg-ANBA-IPA acetate is not typically used in cell-based assays, as it is a substrate for thrombin rather than a modulator of cellular function. However, the substrate can be used in assays measuring thrombin activity in cell culture supernatants or in cell-based models of coagulation. For example, thrombin activity can be measured in the conditioned media of cells that produce thrombin or in co-culture systems. The substrate can also be used to measure the activity of thrombin generated in platelet-rich plasma or whole blood. These assays are useful for studying the regulation of thrombin generation in cellular and physiological contexts.
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| Animal Protocol |
For in vivo animal experiments, Tos-Gly-Pro-Arg-ANBA-IPA acetate 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 thrombin activity in plasma. This approach can be used to evaluate the effects of drug treatments or disease states on thrombin generation and activity in animal models. For example, thrombin 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 thrombin activity in biological samples.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tos-Gly-Pro-Arg-ANBA-IPA acetate 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.
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| Toxicity/Toxicokinetics |
Toxicological data for Tos-Gly-Pro-Arg-ANBA-IPA acetate 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 chromogenic leaving group (ANBA-IPA or related compound) 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.
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| References | |
| Additional Infomation |
Tos-Gly-Pro-Arg-ANBA-IPA acetate is a chromogenic peptide substrate used for measuring thrombin 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 specifically cleaved by thrombin and is used for the detection or measurement of thrombin enzymatic activity. It can be used for luminescence measurement. Tos-Gly-Pro-Arg-ANBA-IPA acetate is a valuable tool for studying coagulation, thrombosis, and for screening thrombin inhibitors.
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| Molecular Formula |
C32H45N9O10S
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|---|---|
| Molecular Weight |
747.819005727768
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| Exact Mass |
747.301
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| CAS # |
2070009-46-8
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| Related CAS # |
Tos-Gly-Pro-Arg-ANBA-IPA;99700-50-2
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| PubChem CID |
92044475
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
52
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| Complexity |
1320
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(=O)(O)C.C([C@@H]1CCCN1C(=O)CNS(C1C=CC(C)=CC=1)(=O)=O)(=O)N[C@@H](CCCNC(N)=N)C(=O)NC1C=CC(N(=O)=O)=C(C(=O)NC(C)C)C=1
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| InChi Key |
RUKOLHFVDDAWSG-CWAVIJBDSA-N
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| InChi Code |
InChI=1S/C30H41N9O8S.C2H4O2/c1-18(2)35-27(41)22-16-20(10-13-24(22)39(44)45)36-28(42)23(6-4-14-33-30(31)32)37-29(43)25-7-5-15-38(25)26(40)17-34-48(46,47)21-11-8-19(3)9-12-21;1-2(3)4/h8-13,16,18,23,25,34H,4-7,14-15,17H2,1-3H3,(H,35,41)(H,36,42)(H,37,43)(H4,31,32,33);1H3,(H,3,4)/t23-,25-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-N-[(2S)-5-(diaminomethylideneamino)-1-[4-nitro-3-(propan-2-ylcarbamoyl)anilino]-1-oxopentan-2-yl]-1-[2-[(4-methylphenyl)sulfonylamino]acetyl]pyrrolidine-2-carboxamide
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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, 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)
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| Solubility (In Vitro) |
H2O : ≥ 25 mg/mL (~33.43 mM)
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| 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 | 1.3372 mL | 6.6861 mL | 13.3722 mL | |
| 5 mM | 0.2674 mL | 1.3372 mL | 2.6744 mL | |
| 10 mM | 0.1337 mL | 0.6686 mL | 1.3372 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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