| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 250mg | |||
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| Targets |
Abz-FR-K(Dnp)-P-OH targets angiotensin I-converting enzyme (ACE). It acts as a specific substrate for this enzyme. The peptide bond between specific amino acids in the FR-K(Dnp) sequence is cleaved by ACE. This cleavage separates the Abz fluorophore from the Dnp quencher, resulting in a measurable increase in fluorescence, making it a valuable tool for studying ACE activity.
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| ln Vitro |
In vitro, Abz-FR-K(Dnp)-P-OH is used to measure the activity of ACE. It is an excellent substrate for ACE, with a reported Km value of 4.0 microM and a kcat value of 210 s-¹. Upon cleavage by ACE, the Abz fluorescence is dequenched, allowing for real-time monitoring of enzyme kinetics. This makes it a highly sensitive tool for characterizing ACE activity, specificity, and the potency of ACE inhibitors.
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| ln Vivo |
Specific in vivo data for Abz-FR-K(Dnp)-P-OH is not applicable as it is a research reagent used in in vitro biochemical assays. It is not intended for in vivo administration or therapeutic use. Its utility lies in providing a robust and sensitive method for studying ACE activity in vitro, which can inform our understanding of the renin-angiotensin system and related cardiovascular physiology.
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| Enzyme Assay |
The in vitro assay using Abz-FR-K(Dnp)-P-OH is a continuous fluorometric assay. The substrate is incubated with the ACE enzyme in an appropriate buffer at 37degC. The reaction progress is monitored in real-time by measuring the increase in fluorescence, typically at excitation/emission wavelengths of approximately 320/420 nm. The initial rate of fluorescence increase is directly proportional to enzyme activity. Kinetic parameters (Km and kcat) and inhibitor potency (IC50) can be determined from the fluorescence data.
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| Cell Assay |
In vitro cellular assays using Abz-FR-K(Dnp)-P-OH are not typically performed because the substrate is designed for use with purified enzyme or in cell lysates. Its application is in biochemical assays to study ACE activity in a controlled environment. For cellular studies, cell lysates containing ACE are prepared and incubated with the substrate to measure the enzyme's activity within the cellular context.
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| Animal Protocol |
In vivo animal studies are not relevant for Abz-FR-K(Dnp)-P-OH as it is an in vitro research tool. The compound is not administered to animals for efficacy or pharmacokinetic studies. Its application is restricted to biochemical and enzymatic research to study ACE function and screen for inhibitors.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not relevant for Abz-FR-K(Dnp)-P-OH, as it is a research reagent used in in vitro assays and not a therapeutic agent. For storage, it is recommended to keep the lyophilized powder at 2-8degC for short-term storage (days to weeks) or at -20degC for long-term storage (months to years). It is soluble in water.
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| Toxicity/Toxicokinetics |
Toxicological data for Abz-FR-K(Dnp)-P-OH is not relevant as it is not a therapeutic compound. As a standard laboratory reagent, it is handled with standard laboratory safety practices. It is explicitly stated that the product is "for non-human research only" and "Not for therapeutic or veterinary use". The compound is not intended for human consumption or exposure.
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| References | |
| Additional Infomation |
Abz-FR-K(Dnp)-P-OH (CAS 500799-61-1) is a widely utilized fluorogenic substrate for angiotensin I-converting enzyme (ACE). It consists of the peptide sequence Abz-Phe-Arg-Lys(Dnp)-Pro-OH. The Abz/Dnp pair acts as a donor-quencher, enabling real-time fluorescence-based assays to study enzyme kinetics and screen for ACE inhibitors. This substrate is a critical tool in cardiovascular research, supporting the development of therapies for conditions like hypertension.
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| Molecular Formula |
C39H49N11O10
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|---|---|
| Molecular Weight |
831.87400
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| Exact Mass |
831.366
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| CAS # |
500799-61-1
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| PubChem CID |
146159019
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.683
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| LogP |
4.12
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
60
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| Complexity |
1510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CCCCNC2=C(C=C(C=C2)[N+](=O)[O-])[N+](=O)[O-])NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)C4=CC=CC=C4N)C(=O)O
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| InChi Key |
ZEWJTBVOMMZVAU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C39H49N11O10/c40-27-13-5-4-12-26(27)34(51)47-31(22-24-10-2-1-3-11-24)36(53)45-29(15-8-20-44-39(41)42)35(52)46-30(37(54)48-21-9-16-32(48)38(55)56)14-6-7-19-43-28-18-17-25(49(57)58)23-33(28)50(59)60/h1-5,10-13,17-18,23,29-32,43H,6-9,14-16,19-22,40H2,(H,45,53)(H,46,52)(H,47,51)(H,55,56)(H4,41,42,44)
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| Chemical Name |
1-[2-[[2-[[2-[(2-aminobenzoyl)amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-6-(2,4-dinitroanilino)hexanoyl]pyrrolidine-2-carboxylic 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 : ≥ 18 mg/mL (~21.64 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 | 1.2021 mL | 6.0106 mL | 12.0211 mL | |
| 5 mM | 0.2404 mL | 1.2021 mL | 2.4042 mL | |
| 10 mM | 0.1202 mL | 0.6011 mL | 1.2021 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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