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P4pal10 is a pepducin antagonist of proteinase-activated receptor 4 (PAR4) and formyl peptide receptor 2 (FPR2), as well as an agonist of free fatty acid receptor 2 (FFAR2/GPR43).{21094,66196} It is composed of a peptide that corresponds to the third intracellular loop of human PAR4 that is conjugated to palmitic acid (Item No. 10006627).{21094} P4pal10 selectively inhibits the aggregation of isolated human platelets induced by the PAR4 peptide agonist AYPGKF-NH2 (Item No. 24258; IC50 = 0.5-1 µM) over the PAR1 peptide agonist SFLLRN-NH2 (Item No. 36881), the TP receptor agonist U-46619 (Item No. 16450), the platelet glycoprotein Ib (GPIb), GPIX, and GPV agonist ristocetin, ADP (Item No. 21121), or collagen at 5 µM. It inhibits increases in intracellular calcium induced by the FPR1 and FPR2 agonist WKYMVm but not by the FPR1 agonist fMLF in isolated human neutrophils and induces superoxide production in TNF-? primed isolated human neutrophils stimulated with the FFAR2 allosteric modulator Cmp58.{66196} P4pal10 (1, 3, or 10 µg/kg) reduces myocardial infarct size in a rat model of coronary artery ligation-induced ischemia-reperfusion injury.{67051} It increases the paw withdrawal threshold in rat models of osteoarthritis induced by monoiodoacetate injection into the knee joint or medial meniscal transection.{66197}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 10 mg, 25 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| Molecular formula | C65H112N22O13 • XCF3COOH |
| Smiles | OC(C=C1)=CC=C1C[C@@H](C(NCC(N[C@H](C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CCCNC(N)=N)=O)=O)=O)CC2=CN=CN2)=O)=O)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC(CNC([C@H](CO)NC(CCCCCCCCCCCCCCC)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O |
| Molecular weight | 1409,7 |
| Custom code | 2933.29 |
| Formulation | A solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
This mixture contains the primary metabolites of prostaglandins (PGs) D2, E2, and F2?. Contents: 13,14-dihydro-15-keto PGD2, 13,14-dihydro-15-keto PGE2, 11?-PGF2?, 13,14-dihydro-15-keto...
To be used in conjunction with Cayman’s NAPE-PLD polyclonal antibody (aa 6-20) (Item No. 10306) to block protein-antibody complex formation...
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The cyclopentenone prostaglandin HPLC mixture contains all of the major UV-absorbing cyclopentenone prostaglandins and their precursors supplied in methyl acetate....
Prostaglandin I synthase (PGIS) catalyzes the isomerization of PGH2 to PGI2. PGI2 (prostacyclin) is a potent vasodilator and inhibitor of...
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This mixture contains the characteristic metabolites of both PGI2 and TXA2. Contents: Thromboxane B2, 11-dehydro Thromboxane B2, 6-keto Prostaglandin F1?,...
The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with an important role in...
Platelet-activating factor (PAF) is an important lipid mediator involved in inflammation. PAF-acetylhydrolase (PAF-AH) is an extracellular phospholipase A2 which hydrolyzes...
Histone H2A is a core histone that forms a dimer with histone H2B.{46631} Two histone H2A/H2B dimers form an octameric...
Inositol hexakisphosphate kinase 2 (IP6K2) is a cytoplasmic kinase that catalyzes the conversion of IP6 to diphosphoinositol pentakisphosphate in the...
GST-tag Polyclonal Antibody (FITC) is a probe for the immunochemical detection of GST tags on recombinant proteins. Recombinant proteins are...
Protein phosphorylation is an important post-translational modification that serves many key functions to regulate a protein’s activity, localization, and protein-protein...
To be used in conjunction with Cayman’s FABP3 polyclonal antibody (Catalog No. 10233) to block protein-antibody complex formation during immunochemical...
TAF10 is one of many protein factors or coactivators associated with RNA polymerase II activity.{16903} One vial of this peptide...
Sirtuin 5 (SIRT5) is an enzyme that catalyzes the NAD-dependent removal of malonyl, succinyl, and glutaryl groups from target proteins.{55107,55108}...
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