| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
VKGILS-NH2 does not have a specific biological target. It is the reverse sequence of the PAR2 activating peptide (SLIGKV). Therefore, it is unable to bind to or activate the protease-activated receptor 2 (PAR2). Its purpose is to act as a negative control to demonstrate that the biological effects observed with SLIGKV-NH2 are specifically due to the peptide sequence and not to non-specific peptide effects (e.g., charge, cytotoxicity).
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|---|---|
| ln Vitro |
VKGILS-NH2 has no biological activity on PAR2 receptors. It is definitively described as having “no effect on DNA synthesis in cells,” confirming its inertness as a control. This lack of activity is expected and serves as the validation for its use.
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| ln Vivo |
Since VKGILS-NH2 is an inactive control peptide, it has no in vivo activity on the PAR2 receptor. It is expected to produce no changes in inflammation, pain response, or smooth muscle contraction, which are the typical endpoints used in PAR2 in vivo models. It is used as a vehicle control for injected peptides.
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| Enzyme Assay |
There is no specific binding protocol for VKGILS-NH2 because it is designed not to bind. Confirmation of its lack of binding is typically done by performing a standard radioligand binding assay using membranes expressing PAR2 and a radiolabeled high-affinity antagonist, demonstrating no displacement of the radioligand by VKGILS-NH2 up to high micromolar concentrations.
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| Cell Assay |
In a standard in vitro cell-based assay, Swiss 3T3 fibroblasts or primary human keratinocytes are cultured and treated with either the PAR2 agonist (SLIGKV-NH2) or the control peptide VKGILS-NH2 at concentrations ranging from 10-500 uM. The cells are then assayed for DNA synthesis, typically by measuring the incorporation of [3H]-thymidine into DNA over a 24-hour period. A significant increase in [3H]-thymidine incorporation is observed with SLIGKV-NH2, whereas VKGILS-NH2 shows no change compared to untreated cells. This procedure validates the specificity of the agonist.
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| Animal Protocol |
There are no specific in vivo protocols for an inactive control peptide. In a typical pain study, the active PAR2 agonist (SLIGKV-NH2) is injected intradermally into the rodent hind paw to induce mechanical hyperalgesia. The control group receives an injection of VKGILS-NH2 at the same volume and concentration (e.g., 100 uM). The paw withdrawal threshold is measured using von Frey filaments. The group receiving VKGILS-NH2 should show no significant difference from the vehicle (saline) control group, while the SLIGKV-NH2 group shows a marked reduction in threshold.
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| ADME/Pharmacokinetics |
VKGILS-NH2 is a simple peptide and is expected to have a short in vivo half-life due to rapid proteolytic degradation by ubiquitous proteases. Its pharmacokinetics are rarely studied, as its only function is to serve as a control to account for non-sequence-specific effects (e.g., injection trauma or peptide solubility issues) in the experimental design.
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| Toxicity/Toxicokinetics |
Toxicity data is not applicable for VKGILS-NH2. As a short, scrambled peptide, it is generally well-tolerated and non-toxic at the concentrations used in experimental protocols (typically 10-500 uM). Any observed adverse events in a control group would be attributed to the solvent or the experimental procedure, not the peptide.
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| References |
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| Additional Infomation |
VKGILS-NH2 is a research-grade peptide used exclusively in cell biology and pharmacology. It is used for: 1) Demonstrating that the effects of SLIGKV-NH2 are not due to the peptide backbone or non-specific interactions. 2) Normalizing data to subtract baseline physiological fluctuations. The amidation (NH2) at the C-terminus increases its stability compared to the free acid form. Its high solubility in water is a beneficial property for reconstitution. It is not a therapeutic agent.
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| Molecular Formula |
C28H54N8O7
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|---|---|
| Molecular Weight |
614.78
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| Exact Mass |
614.412
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| CAS # |
942413-05-0
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| Related CAS # |
VKGILS-NH2 TFA;2828432-41-1
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| PubChem CID |
90488839
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| Appearance |
White to off-white solid powder
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| LogP |
1.779
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
43
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| Complexity |
931
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](C(C)C)N
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| InChi Key |
IYJUKRSADJIIBX-WAUHAFJUSA-N
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| InChi Code |
InChI=1S/C28H54N8O7/c1-7-17(6)23(28(43)34-19(12-15(2)3)26(41)35-20(14-37)24(31)39)36-21(38)13-32-25(40)18(10-8-9-11-29)33-27(42)22(30)16(4)5/h15-20,22-23,37H,7-14,29-30H2,1-6H3,(H2,31,39)(H,32,40)(H,33,42)(H,34,43)(H,35,41)(H,36,38)/t17-,18-,19-,20-,22-,23-/m0/s1
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| Chemical Name |
(2S)-6-amino-N-[2-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-2-[[(2S)-2-amino-3-methylbutanoyl]amino]hexanamide
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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) |
DMSO: 100 mg/mL (162.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6266 mL | 8.1330 mL | 16.2660 mL | |
| 5 mM | 0.3253 mL | 1.6266 mL | 3.2532 mL | |
| 10 mM | 0.1627 mL | 0.8133 mL | 1.6266 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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