| 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 |
PAR-2 (1-6) (SLIGKV) specifically targets and activates the Protease-Activated Receptor 2 (PAR2), a GPCR. It mimics the tethered ligand that is normally revealed after enzymatic cleavage of the receptor's N-terminus by serine proteases (e.g., trypsin, tryptase). This peptide bypasses the need for enzymatic cleavage.
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| ln Vitro |
PAR-2 (1-6) is a potent and selective PAR2 agonist. It effectively activates PAR2 signaling pathways, leading to the mobilization of intracellular calcium, activation of ERK/MAPK kinases, and release of pro-inflammatory cytokines (such as IL-6 and IL-8) in various cell types, including fibroblasts, epithelial cells, and immune cells. Specific EC50 values range from 5-20 uM depending on the assay.
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| ln Vivo |
In vivo, PAR-2 (1-6) (SLIGKV) is used to induce inflammation and pain. Intradermal or intraplantar injection of SLIGKV in rodents induces a rapid and robust inflammatory response characterized by plasma extravasation (edema), mechanical hyperalgesia (increased sensitivity to pain), and neutrophil recruitment. This model is used to study PAR2's role in inflammatory diseases.
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| Enzyme Assay |
The specific binding protocol for a peptide agonist is inferred from functional activity, as radioligand binding assays for PAR2 are challenging due to the large peptide binding interface. A functional binding protocol uses HEK-293 cells expressing human PAR2. Cells are loaded with a calcium dye. Increasing concentrations of SLIGKV (1-200 uM) are added, and the fluorescence increase is measured in real-time. The EC50 is calculated from the concentration-response curve.
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| Cell Assay |
For in vitro assays, primary human lung fibroblasts or HT-29 colon carcinoma cells are cultured in 96-well plates. Following serum starvation, the growth medium is replaced with a buffer containing the calcium indicator Fluo-4 AM. After loading, cells are stimulated with PAR-2 (1-6) peptide (SLIGKV) at concentrations ranging from 5 uM to 200 uM. The resulting intracellular calcium flux is measured using a fluorescence plate reader. Alternatively, cells are treated with 50-100 uM SLIGKV for 4 hours, and IL-8 release in the supernatant is quantified by ELISA.
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| Animal Protocol |
An acute inflammation model is used for in vivo evaluation. Male Swiss-Webster mice (25-30 g) are lightly anesthetized. PAR-2 (1-6) peptide (50-200 uM in 50 uL saline) is injected intradermally into the dorsal skin or intraplantarly into the hind paw. To measure plasma extravasation (edema), Evans Blue dye is injected intravenously prior to the peptide. After 30-60 minutes, the skin patch or paw is excised, and the extravasated dye is extracted and quantified spectrophotometrically. To measure hyperalgesia, paw withdrawal thresholds are measured using von Frey filaments at 15, 30, 60, and 120 minutes post-injection.
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| ADME/Pharmacokinetics |
As a synthetic peptide, PAR-2 (1-6) is rapidly degraded by proteases in vivo, exhibiting a very short plasma half-life (approximately 2-10 minutes). Its activity is highly localized to the site of injection. The rapid degradation is a limiting factor for systemic administration but is acceptable for local dermal applications. Clearance occurs via proteolysis into constituent amino acids, which are recycled.
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| Toxicity/Toxicokinetics |
Toxicity data for PAR-2 (1-6) is limited to the known effects of PAR2 activation. At high systemic doses, over-activation of PAR2 could lead to circulatory failure due to widespread vasodilation and hypotension. However, standard laboratory injections induce only transient, localized inflammation. No chronic toxicity or genotoxicity data is available.
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| References | |
| Additional Infomation |
Derived from the N-terminus of protease-activated receptor 2 (PAR-2)
PAR-2 (1-6) (SLIGKV) is the most widely used experimental tool for activating PAR2 in research settings. It is not a drug and has no clinical approval. It is invaluable for studying the physiological and pathophysiological roles of PAR2 in inflammation, pain, cancer metastasis, and respiratory diseases. The human sequence differs from the rodent (mouse/rat) sequence, which is SLIGRL. Researchers must use the species-specific agonist. The peptide is typically supplied as a TFA salt. |
| Molecular Formula |
C28H53N7O8
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|---|---|
| Molecular Weight |
615.76
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| Exact Mass |
615.396
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| CAS # |
202933-49-1
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| PubChem CID |
10232703
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| Appearance |
White to off-white solid powder
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| LogP |
1.678
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
10
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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)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)N
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| InChi Key |
NTQVODZUQIATFS-WAUHAFJUSA-N
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| InChi Code |
InChI=1S/C28H53N7O8/c1-7-17(6)23(35-26(40)20(12-15(2)3)33-24(38)18(30)14-36)27(41)31-13-21(37)32-19(10-8-9-11-29)25(39)34-22(16(4)5)28(42)43/h15-20,22-23,36H,7-14,29-30H2,1-6H3,(H,31,41)(H,32,37)(H,33,38)(H,34,39)(H,35,40)(H,42,43)/t17-,18-,19-,20-,22-,23-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-methylbutanoic 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: 25 mg/mL (40.60 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 | 1.6240 mL | 8.1200 mL | 16.2401 mL | |
| 5 mM | 0.3248 mL | 1.6240 mL | 3.2480 mL | |
| 10 mM | 0.1624 mL | 0.8120 mL | 1.6240 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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