Recombinant Mouse Proteinase-activated receptor 2 (F2rl1)
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Description
Definition and Overview of Recombinant Mouse Proteinase-Activated Receptor 2 (F2rl1)
Recombinant Mouse Proteinase-Activated Receptor 2 (F2rl1) is a synthetic, laboratory-produced protein corresponding to the mouse homolog of PAR2, a G-protein coupled receptor (GPCR) encoded by the F2rl1 gene. It is engineered for research purposes to study PAR2's roles in inflammation, immune regulation, pain signaling, and cellular signaling pathways. The recombinant protein is typically expressed in prokaryotic systems (e.g., E. coli) and fused with tags (e.g., His, GST) for purification and functional studies .
Protein Structure
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Domain Organization: Full-length recombinant PAR2 includes residues 39–399 (mouse) with a His tag for affinity chromatography .
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Molecular Weight: ~40–42 kDa (varies based on tags and expression systems) .
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Post-Translational Modifications: Includes proteolytic cleavage sites for activation by trypsin, tryptase, or synthetic peptides (e.g., SLIGRL) .
Functional Mechanisms
PAR2 is activated via proteolytic cleavage of its N-terminal domain, exposing a tethered ligand (SLIGKV) that binds to extracellular loop 2 (ECL2) . Key signaling pathways include:
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Mitogen-Activated Protein Kinase (MAPK): Modulates cell migration and proliferation .
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NF-κB/IκB Kinase (IKK): Regulates pro-inflammatory cytokines (e.g., IL-6, IL-8) .
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Rho Kinase: Controls cytoskeletal rearrangement and chemotaxis .
| Pathway | Biological Outcome | Associated Proteases |
|---|---|---|
| PLC → Ca²⁺ signaling | Vasodilation, immune cell activation | Trypsin, tryptase, kallikreins |
| MAPK → Proliferation | Tumor progression, fibrosis | PAR1 transactivation |
| NF-κB → Cytokines | Inflammation, antimicrobial responses | TLR4 synergism |
Analytical and Diagnostic Tools
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ELISA Kits: Quantify F2rl1 levels in mouse serum, plasma, or tissue lysates (detection range: 0.312–20 ng/mL; sensitivity: 0.18 ng/mL) .
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Western Blotting: Validate protein expression and post-translational modifications using His-tagged recombinant PAR2 .
Functional Studies
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Agonist Screening: Synthetic peptides (e.g., SLIGRL) mimic proteolytic activation to study PAR2-mediated responses in immune cells, neurons, and epithelial cells .
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Colitis Models: PAR2 agonists (e.g., SLIGRL-NH₂) reduce TNBS-induced colitis by suppressing IFN-γ and IL-12 production in T lymphocytes .
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Pain Signaling: Conditional knockout mice (F2rl1 flox) reveal PAR2’s role in mechanical allodynia and thermal hyperalgesia via nonpeptidergic DRG neurons .
Inflammatory and Immune Responses
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Anti-Inflammatory Effects: PAR2 activation inhibits JNK phosphorylation and TNF-α signaling, mitigating colitis severity .
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Antimicrobial Activity: Enhances phagocytosis of Gram-positive bacteria and synergizes with IFN-γ to combat viral infections .
Pain and Neurological Signaling
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Neuronal PAR2: Expressed in ~4% of DRG neurons, co-localizing with P2X3 and IL31RA. Activation induces mechanical allodynia via calcium-dependent pathways .
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Non-Neuronal Mechanisms: Endogenous proteases (e.g., neutrophil elastase) mediate thermal hyperalgesia independently of neuronal PAR2 .
Cancer and Metabolic Disorders
Product Specs
Form
Lyophilized powder
Note: We prioritize shipping the format currently in stock. However, if you have specific requirements for the format, please indicate them when placing your order. We will fulfill your request whenever possible.
Note: We prioritize shipping the format currently in stock. However, if you have specific requirements for the format, please indicate them when placing your order. We will fulfill your request whenever possible.
Lead Time
Delivery time
may vary based on the purchasing method or location. Please consult your local distributors
for specific delivery timelines.
Note: All protein shipments are standardly accompanied by blue ice packs. If you require dry ice, please communicate with us in advance. Additional fees will apply.
Note: All protein shipments are standardly accompanied by blue ice packs. If you require dry ice, please communicate with us in advance. Additional fees will apply.
Notes
Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
Reconstitution
We recommend briefly centrifuging this vial before opening to ensure the contents are settled at the bottom. Reconstitute the protein with deionized sterile water to a concentration of 0.1-1.0 mg/mL. We recommend adding 5-50% glycerol (final concentration) and aliquoting for long-term storage at -20°C/-80°C. Our default final glycerol concentration is 50%, which serves as a reference for customers.
Shelf Life
Shelf life is dependent on multiple factors, including storage conditions, buffer components, storage temperature, and the inherent stability of the protein.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
Storage Condition
Upon receipt, store at -20°C/-80°C. Aliquoting is essential for multiple uses. Avoid repeated freeze-thaw cycles.
Tag Info
Tag type is determined during the manufacturing process.
Tag type is determined during production. If you have a specific tag type preference, please let us know, and we will prioritize developing the specified tag.
Synonyms
F2rl1; Gpcr11; Gpr11; Par2; Proteinase-activated receptor 2; PAR-2; Coagulation factor II receptor-like 1; G-protein coupled receptor 11; Thrombin receptor-like 1
Buffer Before Lyophilization
Tris/PBS-based buffer, 6%
Trehalose.
Datasheet
Please contact us to get it.
Expression Region
39-399
Protein Length
Full Length of Mature Protein
Species
Mus musculus (Mouse)
Target Names
Target Protein Sequence
SLIGRLETQPPITGKGVPVEPGFSIDEFSASILTGKLTTVFLPVVYIIVFVIGLPSNGMA
LWIFLFRTKKKHPAVIYMANLALADLLSVIWFPLKISYHLHGNNWVYGEALCKVLIGFFY
GNMYCSILFMTCLSVQRYWVIVNPMGHPRKKANIAVGVSLAIWLLIFLVTIPLYVMKQTI
YIPALNITTCHDVLPEEVLVGDMFNYFLSLAIGVFLFPALLTASAYVLMIKTLRSSAMDE
HSEKKRQRAIRLIITVLAMYFICFAPSNLLLVVHYFLIKTQRQSHVYALYLVALCLSTLN
SCIDPFVYYFVSKDFRDHARNALLCRSVRTVNRMQISLSSNKFSRKSGSYSSSSTSVKTS
Y
Uniprot No.
Target Background
Function
Proteinase-activated receptor 2 (PAR2), also known as F2rl1, is a receptor for trypsin and trypsin-like enzymes coupled to G proteins. Its function is mediated through the activation of several signaling pathways including phospholipase C (PLC), intracellular calcium, mitogen-activated protein kinase (MAPK), I-kappaB kinase/NF-kappaB, and Rho. It can also be transactivated by cleaved F2r/Par1. PAR2 plays a crucial role in modulating inflammatory responses and regulating innate and adaptive immunity. It functions as a sensor for proteolytic enzymes generated during infection. Generally, PAR2 promotes inflammation. It can signal synergistically with Tlr4 and likely Tlr2 in inflammatory responses and modulates Tlr3 signaling. PAR2 also exhibits a protective role in establishing the endothelial barrier, a process involving coagulation factor X. It regulates endothelial cell barrier integrity during neutrophil extravasation, likely following proteolytic cleavage by PRTN3. PAR2 has been proposed to have a bronchoprotective role in airway epithelium, but has also been shown to compromise the airway epithelial barrier by interrupting E-cadherin adhesion. It is involved in the regulation of vascular tone, and its activation results in hypotension, presumably mediated by vasodilation. PAR2 associates with a subset of G protein alpha subunits such as GNAQ, GNA11, GNA14, GNA12, and GNA13, but not with G(o) alpha, G(i) subunit alpha-1, and G(i) subunit alpha-2. PAR2 is believed to be a class B receptor that internalizes as a complex with arrestin and traffics with it to endosomal vesicles, presumably as a desensitized receptor, for extended periods. It mediates inhibition of TNF-alpha stimulated JNK phosphorylation through coupling to GNAQ and GNA11. This function involves dissociation of Ripk1 and Tradd from Tnfr1. PAR2 also mediates phosphorylation of nuclear factor NF-kappa-B RELA subunit at 'Ser-536'. This function involves Ikbkb and is predominantly independent of G proteins. PAR2 is involved in cellular migration. It contributes to cytoskeletal rearrangement and chemotaxis through beta-arrestin-promoted scaffolds. This function is independent of GNAQ and GNA11 and involves promoting cofilin dephosphorylation and actin filament severing. PAR2 induces redistribution of Cops5 from the plasma membrane to the cytosol, and activation of the JNK cascade is mediated by Cops5. It is involved in the recruitment of leukocytes to sites of inflammation and is the primary PAR receptor capable of modulating eosinophil function, including proinflammatory cytokine secretion, superoxide production, and degranulation. During inflammation, it promotes dendritic cell maturation, trafficking to the lymph nodes, and subsequent T-cell activation. PAR2 contributes to the antimicrobial response of innate immune cells, and its activation enhances phagocytosis of Gram-positive bacteria and killing of Gram-negative bacteria. It acts synergistically with interferon-gamma in enhancing antiviral responses.
Gene References Into Functions
- PAR-2 is expressed basolaterally in airway cells, where it stimulates both intracellular Ca(2+) release and Ca(2+) influx, leading to activation of low-level nitric oxide production, increasing apical membrane Cl(-) permeability approximately 3-5-fold, and enhancing ciliary beating by approximately 20-50%. PMID: 28874459
- PAR2 activation in the prostate may contribute to the development of lower urinary tract dysfunction through proinflammatory as well as profibrotic pathways. PMID: 26860791
- Our data indicate that PAR2 counterbalanced enhanced contractions to ET-1 in aortas from Tsk mice. PAR2 could represent a potential target for novel drugs in the treatment of vascular complications associated with fibrosis. PMID: 27625162
- Thrombin is increased in a mouse model of cancer cachexia in a partially interleukin-6 dependent manner. PMID: 28058802
- Data demonstrate that activated protein C signals via protease activated receptors PAR2/PAR3 to expand Treg cells, mitigating the disease in mice. PMID: 28827518
- PAR2 plays a significant and previously unrecognized anti-apoptotic role in T cell development. PMID: 28951199
- Thrombin has a role in diet-induced obesity through fibrin-driven inflammation. PMID: 28737512
- Data show that PAR2 modulation was sufficient to induce islet cell transdifferentiation in the absence of beta-cells. PMID: 27809303
- Our results suggest that PAR2 inhibition may play a role in the treatment of diseases characterized by increased inflammatory responses in renal systems. PMID: 28694352
- PAR2/GSK3beta is a novel pathway that plays a critical role in the regulation of stem/progenitor cell survival and proliferation in normal colon crypts and colon cancer. PMID: 27313176
- PAR2 is critically important in the pathogenesis of adenine-induced tubular injury. PMID: 28025140
- The levels of miR-223, miR-339, and miR-21, which are associated with platelet activation, were elevated in pooled mouse plasma exosomes before thrombosis and enriched in thrombin-stimulated platelet-derived exosomes in vitro. PMID: 27198239
- Neutrophil elastase induced acute inflammation and pain in knee joints of mice. These changes are PAR2-dependent and appear to involve activation of a p44/42 MAPK pathway. Blocking neutrophil elastase, PAR2, and p44/42 MAPK activity can reduce inflammation and pain, suggesting their utility as therapeutic targets. PMID: 26140667
- Reductions in astrogliosis, inflammation, and neuromotor recovery observed in protease Activated Receptor 2 knockout mice after spinal cord injury suggest that this receptor and its agonists represent new drug targets to promote neuromotor recovery. PMID: 26316358
- Stimulation of PAR-2 activates Nf-kappaB signaling, resulting in RelA nuclear translocation and enhanced expression of pro-inflammatory mRNAs in oral squamous cell carcinoma. PMID: 26839311
- Tryptase and protease-activated receptor-2 stimulate scratching behavior in a murine model of ovalbumin-induced atopic-like dermatitis. PMID: 26049029
- This study reveals, for the first time, an important role for PAR2 in allergic lung inflammation. PMID: 24048772
- HAI-1 may play a critical role in maintaining normal keratinocyte morphology through regulation of PAR-2-dependent p38 mitogen-activated protein kinase signaling. PMID: 25842366
- PAR2 activation through endogenous mast cell tryptase activity could be required, at least partially, to mediate CCL11-induced eosinophil migration. PMID: 24972241
- These studies identify the thrombin receptor as a powerful extracellular regulatory switch that could be readily targeted to improve myelin production in the face of white matter injury and disease. PMID: 25628003
- PAR2 knockout prevented bone cancer-related pain behaviors and associated neurochemical changes in dorsal root ganglion and dorsal horn. PMID: 23893658
- TR deficiency inhibits osteoclastogenesis by decreasing RANKL/OPG ratio, resulting in a high bone mass phenotype. PMID: 25460576
- These findings indicate that hematopoietic TF-PAR2 signaling plays a pivotal role in the hepatic inflammatory responses, steatosis, and hepatic insulin resistance that lead to systemic insulin resistance and type 2 diabetes in obesity. PMID: 25476527
- Findings unveil an important mechanism by which IL-1beta regulates its own endothelial cytotoxic actions by augmenting neuronal Par2 expression to repress sequentially IL-1 receptor type I and Sema3A expression. PMID: 25478809
- Data suggest that proteinase-activated receptor 2 activation leads to up-regulation of the dual oxidase-2/reactive oxygen species pathway in airway epithelial cells (AECs). PMID: 25684443
- Data show that proteinase-activated receptor (PAR)-2-dependent inflammatory signaling is an essential component of matriptase-mediated and potentiation of ras-mediated oncogenesis. PMID: 24469043
- Serine proteases and protease-activated receptor 2 mediate the proinflammatory and algesic actions of diverse stimulants. PMID: 24749982
- Deletion of PAR-2 results in a significant decrease in medial meniscus destabilization-induced cartilage damage. Chondroprotection appears to occur through modulation of extracartilaginous events. PMID: 25200274
- PAR2 was required for the development of chronic pelvic pain in experimental autoimmune prostatitis. PMID: 24726923
- The role of PAR-2 activation in allergic sensitization and house dust mite-induced allergic airway inflammation was investigated. PMID: 24651123
- Mutant versions of F2rl1 that prevent nuclear relocalization but not plasma membrane activation interfere with Vegfa but not Ang1 expression. Complementary factors are therefore regulated by the subcellular localization of F2rl1, which governs angiogenesis. PMID: 25216639
- PAR-2 signaling contributes to the pathogenesis of hypertrophy and heart failure. PMID: 24312345
- It triggers pancreatic nociception. PMID: 24162021
- The present study demonstrates that Klk6 signals through PAR1 to regulate oligodendrocyte process stability and extension, myelin gene expression, and cell survival in the presence of oligotoxic agents. PMID: 23832758
- PAR2 synergizes with the TGFbeta signaling pathway to contribute to renal injury and fibrosis. PMID: 24253040
- PAR2 signaling is required for hyperexcitability of colonic nociceptive DRG neurons induced by colonic supernatant of diarrhea-predominant irritable bowel syndrome patients. PMID: 23958521
- Data suggest a tissue factor (TF) and protease-activated receptor 2 (PAR-2)-dependent mechanism on dexamethasone-dendritic cells (DC) in vitro and unprimed DC in vivo that contributes to the low immunogenicity of these cells. PMID: 23347132
- Cross-talk between PAR2 and TLR4 contributes to vascular homeostasis. PMID: 22957757
- Renal proteinase-activated receptor 2 has a role in the control of blood pressure and plasma potassium level. PMID: 23430254
- Mast cell/chymase-mediated intestinal epithelial barrier function is mediated by proteinase-activated receptor 2/matrix metallopeptidase 2-dependent. PMID: 23306080
- Protease-activated receptor 2 (PAR2) protein and transient receptor potential vanilloid 4 (TRPV4) protein coupling is required for sustained inflammatory signaling. PMID: 23288842
- Mast cell degranulation with subsequent release of tryptase and protease-activated receptor 2 activation are potential targets for the development of novel therapies to prevent, but not reverse, postoperative pain. PMID: 23249992
- Mainly through its serine protease activity, the house dust mite potentiates capsaicin-evoked transiently divalent calcium-ion levels in mouse pulmonary sensory neurons via activation of PAR2. PMID: 22125310
- Protease-activated receptor 2 mediates mucus secretion in the airway submucosal gland. PMID: 22916223
- Data suggest that the proteinase-activated receptor-2 PAR(2)-enhanced inflammatory process is beta-arrestin-2 dependent, whereas the protective anticonstrictor effect of bronchial epithelial PAR(2) may be beta-arrestin independent. PMID: 23012429
- A direct role is found for PAR2 transgene in acute cancer pain in an animal model of head and neck cancer. PMID: 23055487
- Deletion of protease-activated receptor 2 prolongs the survival of scrapie in a mouse model. PMID: 22694901
- These data support an important role for PAR(2) in the pathogenesis of collagen-induced arthritis model. PMID: 22563031
- Analysis of the metastatic potential of B16 melanoma in knock-out (PAR2-/-) animals. PMID: 22578959
- These results suggest that PAR(2) activation contributes to the determination of cells of both osteoblast and osteoclast lineages within bone marrow, and thereby participates in the regulation of skeletal growth and bone repair. PMID: 22173052
Database Links
Protein Families
G-protein coupled receptor 1 family
Subcellular Location
Cell membrane; Multi-pass membrane protein.
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