| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: = 99%
| Targets |
The primary targets of Pyr-Arg-Thr-Lys-Arg-AMC TFA are proteases, particularly trypsin and thrombin. The peptide sequence is specifically recognized and hydrolyzed by these enzymes. The compound is used to determine the activity of proteases and the potency of enzyme inhibitors. Its specificity for certain proteases makes it a valuable tool for studying protease function and screening inhibitors.
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| ln Vitro |
In vitro activity of Pyr-Arg-Thr-Lys-Arg-AMC TFA is measured by its hydrolysis by target proteases. The compound is incubated with protease enzymes, and the release of fluorescent AMC is monitored over time. The rate of fluorescence increase is proportional to protease activity. This assay is used to determine the kinetic parameters of protease enzymes and to screen for protease inhibitors.
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| ln Vivo |
In vivo activity data for Pyr-Arg-Thr-Lys-Arg-AMC TFA are not applicable, as the compound is a research reagent used in biochemical assays rather than a therapeutic agent. It is not administered to animals or humans. Its use is limited to in vitro enzymatic assays for studying protease activity and inhibitor potency.
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| Enzyme Assay |
Non-cellular assays for Pyr-Arg-Thr-Lys-Arg-AMC TFA involve incubating the compound with purified protease enzymes in buffer solutions. The release of fluorescent AMC is monitored using a fluorescence spectrophotometer with excitation at approximately 360 nm and emission at approximately 460 nm. The reaction rate is calculated from the linear portion of the fluorescence versus time curve. IC50 values for inhibitors are determined by testing a range of inhibitor concentrations.
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| Cell Assay |
Cellular assays for Pyr-Arg-Thr-Lys-Arg-AMC TFA are not typically conducted, as the compound is used in cell-free enzymatic assays. The compound is membrane-impermeant and is not suitable for intracellular studies. Its use is limited to in vitro applications where purified proteases or cell lysates are used as the enzyme source.
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| Animal Protocol |
In vivo animal experiments are not conducted for Pyr-Arg-Thr-Lys-Arg-AMC TFA, as it is a research reagent for biochemical assays rather than a therapeutic compound. The compound is not administered to animals for any research purpose. Its applications are strictly limited to in vitro enzymatic studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not applicable for Pyr-Arg-Thr-Lys-Arg-AMC TFA, as it is a research reagent and not a pharmaceutical compound. The compound is soluble in water (90 mg/mL) and should be stored at -20°C protected from light, dry, and sealed. It is stable under these storage conditions. The compound's large molecular weight (941.95 g/mol) and peptide nature limit its membrane permeability.
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| Toxicity/Toxicokinetics |
Toxicological data for Pyr-Arg-Thr-Lys-Arg-AMC TFA are limited, as it is a research reagent not intended for human or animal use. Standard laboratory safety precautions should be followed when handling this compound. It may be irritating to skin, eyes, and respiratory tract. Appropriate personal protective equipment should be worn when handling the compound.
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| References | |
| Additional Infomation |
Other information includes the compound's use as a fluorogenic substrate for protease assays. It is selectively cleaved by proteases such as trypsin and thrombin, releasing the fluorescent AMC group. The compound is used to determine protease activity and assess enzyme inhibitor potency. It is an AMC-tagged decapeptide with the sequence Pyr-Arg-Thr-Lys-Arg-AMC. The compound is stored at -20°C protected from light.
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| Molecular Formula |
C39H58F3N13O11
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|---|---|
| Molecular Weight |
941.953538417816
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| Exact Mass |
941.433
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| CAS # |
1255501-99-5
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| Related CAS # |
Pyr-Arg-Thr-Lys-Arg-AMC;155575-02-3
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| PubChem CID |
71311915
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
66
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| Complexity |
1680
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| Defined Atom Stereocenter Count |
6
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| SMILES |
FC(C(=O)O)(F)F.O[C@H](C)[C@@H](C(N[C@H](C(N[C@H](C(NC1=CC=C2C(C)=CC(=O)OC2=C1)=O)CCC/N=C(\N)/N)=O)CCCCN)=O)NC([C@H](CCC/N=C(\N)/N)NC([C@@H]1CCC(N1)=O)=O)=O
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| InChi Key |
BHPUHMHLXQHSPN-HUQKKSBQSA-N
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| InChi Code |
InChI=1S/C37H57N13O9.C2HF3O2/c1-19-17-29(53)59-27-18-21(10-11-22(19)27)45-31(54)24(8-5-15-43-36(39)40)47-32(55)23(7-3-4-14-38)49-35(58)30(20(2)51)50-34(57)25(9-6-16-44-37(41)42)48-33(56)26-12-13-28(52)46-26;3-2(4,5)1(6)7/h10-11,17-18,20,23-26,30,51H,3-9,12-16,38H2,1-2H3,(H,45,54)(H,46,52)(H,47,55)(H,48,56)(H,49,58)(H,50,57)(H4,39,40,43)(H4,41,42,44);(H,6,7)/t20-,23+,24+,25+,26+,30+;/m1./s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S,3R)-1-[[(2S)-6-amino-1-[[(2S)-5-(diaminomethylideneamino)-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-oxopyrrolidine-2-carboxamide;2,2,2-trifluoroacetic 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) |
H2O: 100 mg/mL (106.16 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 | 1.0616 mL | 5.3081 mL | 10.6163 mL | |
| 5 mM | 0.2123 mL | 1.0616 mL | 2.1233 mL | |
| 10 mM | 0.1062 mL | 0.5308 mL | 1.0616 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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