| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide targets human enteropeptidase (enterokinase), a serine protease that plays a critical role in the activation of pancreatic enzymes. Enteropeptidase cleaves the peptide bond after the lysine residue in the sequence (Asp)4-Lys, which is the activation sequence of trypsinogen. The peptide substrate GD4K-na is designed to mimic this natural cleavage site and is specifically recognized and cleaved by enteropeptidase, making it a valuable tool for enzyme activity assays.
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|---|---|
| ln Vitro |
At a rate of Km: 0:16 mM and kcat: 115 seconds, purified recombinant human intestinal peptidase light chain (L-HEP) cleaves Gly-Asp-Asp-Asp-Lys-β-naphthylamide [1].
In vitro, Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide serves as a substrate for human enteropeptidase with a Km value of 0.16 mM. Upon cleavage by enteropeptidase, the peptide releases the fluorogenic or chromogenic β-naphthylamide moiety, which can be quantified to measure enzyme activity. The compound is not a therapeutic agent but rather a research tool for studying enteropeptidase function, screening for enteropeptidase inhibitors, and characterizing the enzyme's substrate specificity. |
| ln Vivo |
Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide does not have direct in vivo pharmacological activity as a therapeutic agent. It is a research tool used for in vitro enzymatic assays. In vivo, the peptide would likely be rapidly degraded by proteases. Its primary application is in the development of assays for enteropeptidase activity in biological samples or for screening compounds that modulate enteropeptidase function.
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| Enzyme Assay |
In vitro enzyme assays using Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide typically involve incubating the peptide substrate with human enteropeptidase in a suitable buffer at optimal pH and temperature. The release of β-naphthylamide is monitored continuously using fluorescence (excitation ~340 nm, emission ~410 nm) or at specific time points after stopping the reaction. The rate of substrate hydrolysis is used to calculate enzyme activity, and kinetic parameters such as Km and Vmax can be determined from substrate concentration curves.
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| Cell Assay |
In vitro cell-based assays for Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide are not typically performed, as the peptide is a substrate for enzymatic assays rather than a cell-permeable compound. If used in cell-based systems, the peptide would need to be delivered to cells or used in cell lysates to measure intracellular or secreted enteropeptidase activity. Standard cell culture and lysis protocols would be employed, followed by the fluorogenic substrate assay as described above.
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| Animal Protocol |
In vivo animal studies for Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide are not conducted, as the compound is a research reagent rather than a therapeutic or diagnostic agent. The peptide is used exclusively for in vitro enzymatic assays to study enteropeptidase activity. No animal studies have been reported for this compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide are not relevant, as the compound is not intended for in vivo administration. As a peptide, it would be rapidly degraded by proteases if administered in vivo, and it would not be orally bioavailable. The compound is used exclusively as an in vitro research reagent for enzymatic assays.
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| Toxicity/Toxicokinetics |
The toxicity profile of Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide has not been evaluated, as the compound is not intended for in vivo use. As a peptide, it is expected to have low toxicity in vitro at the concentrations used for enzymatic assays (typically micromolar range). Standard laboratory precautions for handling peptides should be observed. No specific toxicity data are available.
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| References | |
| Additional Infomation |
Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide (GD4K-na) is a synthetic peptide substrate for human enteropeptidase. It has the sequence Gly-Asp-Asp-Asp-Asp-Lys-β-naphthylamide and a molecular weight of 788.76. The peptide mimics the natural trypsinogen activation sequence and is specifically cleaved by enteropeptidase with a Km of 0.16 mM. It is used as a research tool for studying enteropeptidase activity, screening for inhibitors, and characterizing enzyme specificity. The compound is not approved for clinical use.
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| Molecular Formula |
C34H44N8O14
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|---|---|
| Molecular Weight |
788.76
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| Exact Mass |
788.298
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| CAS # |
70023-02-8
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| PubChem CID |
172458
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| Appearance |
White to off-white solid powder
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| Density |
1.468g/cm3
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| Boiling Point |
1378.8ºC at 760 mmHg
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| Flash Point |
787.7ºC
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| Index of Refraction |
1.631
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| LogP |
0.616
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
56
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| Complexity |
1460
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=CC=C2C=C(C=CC2=C1)NC(=O)[C@H](CCCCN)NC(=O)C(CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)CN
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| InChi Key |
QLLWULMEPVZWTP-VPRBCIFISA-N
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| InChi Code |
InChI=1S/C34H44N8O14/c35-10-4-3-7-20(30(52)37-19-9-8-17-5-1-2-6-18(17)11-19)39-32(54)22(13-27(46)47)41-34(56)24(15-29(50)51)42-33(55)23(14-28(48)49)40-31(53)21(12-26(44)45)38-25(43)16-36/h1-2,5-6,8-9,11,20-24H,3-4,7,10,12-16,35-36H2,(H,37,52)(H,38,43)(H,39,54)(H,40,53)(H,41,56)(H,42,55)(H,44,45)(H,46,47)(H,48,49)(H,50,51)/t20-,21-,22?,23-,24-/m0/s1
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| Chemical Name |
(3S)-3-[(2-aminoacetyl)amino]-4-[[(2S)-1-[[(2S)-1-[[1-[[(2S)-6-amino-1-(naphthalen-2-ylamino)-1-oxohexan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-oxobutanoic 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.2678 mL | 6.3391 mL | 12.6781 mL | |
| 5 mM | 0.2536 mL | 1.2678 mL | 2.5356 mL | |
| 10 mM | 0.1268 mL | 0.6339 mL | 1.2678 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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