P4pal10 (trifluoroacetate salt)
(Synonyms: Palmitoyl-SGRRYGHALR-amide, Palmitoyl-SGRRYGHALR-NH2) 目录号 : GC52342A PAR4 and FPR2 antagonist and an FFAR2 agonist
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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)
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。