| 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 |
| Targets |
LRGILS-NH2 TFA does not have a biological target. It is a negative control peptide, meaning it is structurally similar to the active peptide (SLIGRL-NH2) but does not bind to or activate the protease-activated receptor-2 (PAR-2).
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| ln Vitro |
LRGILS-NH2 TFA is a negative control peptide for PAR-2 studies. It is the reverse sequence of SLIGRL-NH2 and is inactive at PAR-2. It is used to confirm that the effects observed with SLIGRL-NH2 are specific to PAR-2 activation and not due to non-specific peptide effects.
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| ln Vivo |
LRGILS-NH2 TFA has no in vivo activity because it is specifically designed as an inactive control. It is not intended to produce any pharmacological response. It is used to control for non-specific effects of the active peptide in in vivo experiments.
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| Enzyme Assay |
Non-cell binding assays are not performed for the inactive control peptide itself, as it is defined by its lack of activity. Instead, PAR-2 binding studies would be performed with the active agonist SLIGRL-NH2. Briefly, purified PAR-2 receptor (often in membrane preparations from PAR-2-expressing cells) is incubated with radiolabeled agonist (e.g., [3H]-SLIGRL-NH2) in the presence of increasing concentrations of unlabeled SLIGRL-NH2 (active) or LRGILS-NH2 (control). LRGILS-NH2 would show no significant displacement of the radiolabeled ligand, confirming its lack of binding.
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| Cell Assay |
LRGILS-NH2 TFA is used in cell-based assays as a negative control alongside the active PAR-2 agonist SLIGRL-NH2. The same cell types and assay conditions are used for both peptides. For cell-based activity assays, cells endogenously expressing PAR-2 (e.g., human keratinocytes, endothelial cells, or smooth muscle cells) or PAR-2-transfected cell lines are seeded in 96-well plates. Cells are treated with LRGILS-NH2 TFA (control) or SLIGRL-NH2 (active) at the same concentration range (e.g., 1-100 uM) for the same duration (e.g., 30-60 minutes). A PAR-2-specific antagonist (e.g., ENMD-1068 or I-191) can be used as a control for specificity. Readouts can include intracellular calcium mobilization (using Fluo-4 AM), ERK phosphorylation (by Western blotting or phospho-ERK ELISA), or gene expression (e.g., IL-6, IL-8, COX-2 by qRT-PCR). Cytokine secretion (IL-6, IL-8) is measured in the supernatants by ELISA. The control peptide should not induce any of these responses. Alternatively, for cell proliferation assays, cells are treated with the peptides for 24-72 hours, and viability is measured by MTT.
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| Animal Protocol |
In vivo animal studies using LRGILS-NH2 TFA are performed as a negative control alongside SLIGRL-NH2 in rodent models of inflammation, pain, or wound healing. For example, in a mouse model of acute inflammation, 6-8 week old female BALB/c or C57BL/6 mice are used. LRGILS-NH2 TFA and SLIGRL-NH2 are injected intraplantarly into the mouse paw (10-100 ug/paw in 20-50 uL saline) or applied topically. Paw swelling is measured using a caliper or plethysmometer before injection and at various time points (0, 1, 2, 4, 6, 8, 12, 24 hours) post-injection. In a model of colitis (DSS-induced), mice receive intrarectal administration of the peptides. The inactive control peptide should not induce inflammation, increase cytokine levels, or cause other PAR-2-mediated effects. Blood and tissue samples are collected for histopathology and cytokine analysis. For pain studies, the peptides are injected intrathecally (into the spinal cord) or intraplantarly, and pain behaviors (mechanical allodynia, thermal hyperalgesia) are assessed. The data from the LRGILS-NH2 TFA group are used as a baseline to subtract from the SLIGRL-NH2 group to determine the specific effects of PAR-2 activation.
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| ADME/Pharmacokinetics |
LRGILS-NH2 TFA is an inactive control peptide. As such, its pharmacokinetic properties are not of interest. It is a small peptide (MW ~770.84 Da) that is expected to be rapidly cleared from circulation and metabolized. The TFA salt form improves solubility. It is not intended for pharmacokinetic or efficacy studies, but rather to validate experimental results from the active compound.
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| Toxicity/Toxicokinetics |
As an inactive control peptide, LRGILS-NH2 TFA is expected to be non-toxic at the concentrations used in experiments (typically <100 uM in vitro, <100 ug/paw in vivo). In controlled studies, it does not produce the adverse effects observed with the PAR-2 agonist (which can include inflammation, pain, and other side effects). No specific toxicity studies have been conducted. Standard safety precautions apply.
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| References | |
| Additional Infomation |
LRGILS-NH2 TFA is a research-grade peptide used as a negative control in experiments involving PAR-2 (Protease-Activated Receptor 2). Its primary use is to control for the non-specific effects of the PAR-2 activating peptide SLIGRL-NH2. It has no known therapeutic use and has not received regulatory approval. The TFA salt is used to enhance solubility and stability. It is strictly for research use only.
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| Molecular Formula |
C31H57F3N10O9
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|---|---|
| Molecular Weight |
770.84
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| Related CAS # |
LRGILS-NH2;245329-01-5
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| Appearance |
White to off-white solid powder
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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 (~129.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.24 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2973 mL | 6.4864 mL | 12.9729 mL | |
| 5 mM | 0.2595 mL | 1.2973 mL | 2.5946 mL | |
| 10 mM | 0.1297 mL | 0.6486 mL | 1.2973 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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