P4pal10 (trifluoroacetate salt) (Synonyms: Palmitoyl-SGRRYGHALR-amide, Palmitoyl-SGRRYGHALR-NH2) |
| Katalog-Nr.GC52342 |
A PAR4 and FPR2 antagonist and an FFAR2 agonist
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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).1,2 It is composed of a peptide that corresponds to the third intracellular loop of human PAR4 that is conjugated to palmitic acid .1 P4pal10 selectively inhibits the aggregation of isolated human platelets induced by the PAR4 peptide agonist AYPGKF-NH2 over the PAR1 peptide agonist SFLLRN-NH2 , the TP receptor agonist U-46619 , the platelet glycoprotein Ib (GPIb), GPIX, and GPV agonist ristocetin, ADP , 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-α primed isolated human neutrophils stimulated with the FFAR2 allosteric modulator Cmp58.2 P4pal10 (1, 3, or 10 µg/kg) reduces myocardial infarct size in a rat model of coronary artery ligation-induced ischemia-reperfusion injury.3 It increases the paw withdrawal threshold in rat models of osteoarthritis induced by monoiodoacetate injection into the knee joint or medial meniscal transection.4
1.Covic, L., Misra, M., Badar, J., et al.Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activationNat. Med.8(10)1161-1165(2002) 2.Holdfeldt, A., Lind, S., Hesse, C., et al.The PAR4-derived pepducin P4Pal10 lacks effect on neutrophil GPCRs that couple to Gαq for signaling but distinctly modulates function of the Gαi-coupled FPR2 and FFAR2Biochem Pharmacol.114143(2020) 3.Strande, J.L., Hsu, A., Su, J., et al.Inhibiting protease-activated receptor 4 limits myocardial ischemia/reperfusion injury in rat hearts by unmasking adenosine signalingJ. Pharmacol. Exp. Ther.324(3)1045-1054(2008) 4.O'Brien, M.S., and McDougall, J.J.Targeting proteinase activated receptor-4 reduces mechanonociception during the acute inflammatory phase but not the chronic neuropathic phase of osteoarthritis in ratsFront. Pharmacol.12756632(2021)
| Cas No. | SDF | ||
| Überlieferungen | Palmitoyl-SGRRYGHALR-amide, Palmitoyl-SGRRYGHALR-NH2 | ||
| Canonical 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 | ||
| Formula | C65H112N22O13 ? XCF3COOH | M.Wt | 1409.7 |
| Löslichkeit | DMF: insol,DMSO: insol,Ethanol: insol,PBS (pH 7.2): 1 mg/ml | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.7094 mL | 3.5469 mL | 7.0937 mL |
| 5 mM | 0.1419 mL | 0.7094 mL | 1.4187 mL |
| 10 mM | 0.0709 mL | 0.3547 mL | 0.7094 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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