| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
PAR-2 AP selectively targets the protease-activated receptor 2 (PAR-2). It binds to the receptor and activates it by acting as a tethered ligand, mimicking the effect of proteolytic cleavage by trypsin or other proteases. It does not activate other PAR subtypes.
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|---|---|
| ln Vitro |
SLIGRL-NH2 is an agonist of PAR-2 and MrgprC11 [1]. SLIGRL-NH2 inhibits L-NAME inhibition. SLIGRL-NH2 causes concentration-induced stress in endothelial cells in the presence of perivascular adipose tissue (PVAT), with an EC50 of 10 μM. Therefore, 20 μM is an acceptable "test" concentration for the peptide in other impact investigations. Designed to evaluate the preparational nature of ADRF release/action. In endothelium-free aortic formulations, SLIGRL-NH2 produces concentration contraction only when PVAT is present [+PVAT, -ENDO(endothelium)] [2].
In vitro, PAR-2 AP activates PAR-2 in various cell types, including endothelial cells, epithelial cells, and smooth muscle cells. Activation leads to calcium mobilization, ERK phosphorylation, and the production of inflammatory mediators such as cytokines and prostaglandins. It has EC50 values in the micromolar range. |
| ln Vivo |
In vivo, PAR-2 AP has been shown to induce inflammation, pain, and vasodilation in animal models. It is used to study the role of PAR-2 in various diseases, including arthritis, asthma, and gastrointestinal disorders. It is also used to study the role of PAR-2 in pain and itch.
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| Enzyme Assay |
In vitro receptor activation assays are performed using cells expressing PAR-2. Cells are loaded with a calcium-sensitive fluorescent dye, and changes in intracellular calcium are measured upon addition of PAR-2 AP. Alternatively, ERK phosphorylation is measured by Western blot.
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| Cell Assay |
Cells (e.g., HEK293 cells transfected with PAR-2) are cultured. Cells are loaded with Fluo-4 or Fura-2. Various concentrations of PAR-2 AP are added, and fluorescence is measured using a fluorescence plate reader. The EC50 is calculated from the dose-response curve.
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| Animal Protocol |
Animal studies use rodent models. PAR-2 AP is administered via intradermal, intraperitoneal, or intracerebroventricular injection. Paw edema is measured to assess inflammation. Pain is assessed by measuring withdrawal thresholds. Vascular permeability is assessed by Evans blue extravasation.
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| ADME/Pharmacokinetics |
PAR-2 AP is a peptide with the sequence SLIGRL-NH2 (MW 700.88). It is typically administered by injection due to poor oral bioavailability. It has a short half-life in vivo due to proteolytic degradation.
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| Toxicity/Toxicokinetics |
PAR-2 AP is generally well-tolerated at pharmacologically active doses. No significant toxicity has been reported. Comprehensive toxicological data are limited. It is a research compound and not intended for human use.
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| References |
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| Additional Infomation |
PAR-2 AP is a research tool used to study PAR-2 biology. It is not an approved drug and is not in clinical trials. It is widely used in pharmacological studies to characterize the role of PAR-2 in health and disease. It is also known as SLIGRL-NH2.
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| Molecular Formula |
C29H56N10O7
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|---|---|
| Molecular Weight |
656.81774
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| Exact Mass |
656.433
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| CAS # |
171436-38-7
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| Related CAS # |
SLIGRL-NH2 TFA;2828432-39-7
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| PubChem CID |
9831050
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| Appearance |
White to off-white solid powder
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| Density |
1.342g/cm3
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| LogP |
1.794
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
46
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| Complexity |
1050
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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](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)N
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| InChi Key |
SGPMJRPYYIJZPC-JYAZKYGWSA-N
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| InChi Code |
InChI=1S/C29H56N10O7/c1-7-17(6)23(39-27(45)21(12-16(4)5)38-25(43)18(30)14-40)28(46)35-13-22(41)36-19(9-8-10-34-29(32)33)26(44)37-20(24(31)42)11-15(2)3/h15-21,23,40H,7-14,30H2,1-6H3,(H2,31,42)(H,35,46)(H,36,41)(H,37,44)(H,38,43)(H,39,45)(H4,32,33,34)/t17-,18-,19-,20-,21-,23-/m0/s1
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| Chemical Name |
(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-N-[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-methylpentanamide
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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) |
H2O : ~110 mg/mL (~167.47 mM)
DMSO : ~100 mg/mL (~152.25 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.81 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 (3.81 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 (3.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (152.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5225 mL | 7.6124 mL | 15.2249 mL | |
| 5 mM | 0.3045 mL | 1.5225 mL | 3.0450 mL | |
| 10 mM | 0.1522 mL | 0.7612 mL | 1.5225 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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