FSLLRY-NH2
目录号 : GC10790
FSLLRY-NH2是蛋白酶激活受体2（PAR-2）的拮抗剂。
Cas No.:245329-02-6
Sample solution is provided at 25 µL, 10mM.
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FSLLRY-NH2 is an antagonist of the protease-activated receptor 2 (PAR-2) [1]. FSLLRY-NH2 inhibits receptor activation by binding to the external loop 2 (ECL-2) region of PAR-2, thereby blocking protease-induced signal transduction [2]. FSLLRY-NH2 applications in research on inflammation, pruritus, and immune responses [3-4].
In HepG2 cells, FSLLRY-NH2 (100-300μM; 24h) reduces the level of the pro-inflammatory genes IL-8, IL-1b, and TNF-α induced by H2O2, through the SAPK/JNK pathways [5]. In A549 cells, FSLLRY-NH2 (100μM; 24h) inhibits PAR2 expression in cells [6].
In asphyxial cardiac arrest (ACA)-induced rat model, FSLLRY-NH2 (50µg; nas; single administration) treatment significantly improved neurological outcomes and reduced the number of degenerating hippocampal neurons after ACA [7]. In Ren-TG mice, FSLLRY-NH2 (10μg/kg; sc; 4 weeks) treatment attenuated the increase in total cardiac mRNA expression of PAR-2, β-MHC, COL3A1, and TGF-β1 [8].
References:
[1]. Ocasio-Rivera M, Marin-Maldonado F, Trossi-Torres G, et al. Targeting of protease activator receptor-2 (PAR-2) antagonist FSLLRY-NH2 as an asthma adjuvant therapy[J]. Medicine, 2020, 99(43): e22351.
[2]. Hughes K H. Effects of chronic subcutaneous adminstered proteinase-activated receptor 2-activating peptide on vascular reactivity of aortas and blood pressures in mice[D]. Memorial University of Newfoundland, 2011.
[3]. Tsagareli M G, Follansbee T, Iodi Carstens M, et al. Targeting transient receptor potential (TRP) channels, Mas-related G-protein-coupled receptors (Mrgprs), and protease-activated receptors (PARs) to relieve itch[J]. Pharmaceuticals, 2023, 16(12): 1707.
[4]. Weng H J, Pham Q T T, Chang C W, et al. Druggable Targets and Compounds with Both Antinociceptive and Antipruritic Effects[J]. Pharmaceuticals, 2022, 15(7): 892.
[5]. Lee Y J, Kim S J, Kwon K W, et al. Inhibitory effect of FSLLRY-NH2 on inflammatory responses induced by hydrogen peroxide in HepG2 cells[J]. Archives of Pharmacal Research, 2017, 40(7): 854-863.
[6]. Wang B, Wu M D, Lan Y J, et al. PAR2 promotes malignancy in lung adenocarcinoma[J]. American Journal of Translational Research, 2024, 16(12): 7416.
[7]. Ocak U, Ocak P E, Huang L, et al. FSLLRY-NH2 improves neurological outcome after cardiac arrest in rats[J]. Turk Neurosurg, 2020, 30(2): 244-251.
[8]. Narita M, Hanada K, Yokono Y, et al. P938 A direct factor Xa inhibitor, rivaroxaban, attenuates cardiac hypertrophy and fibrosis in renin-overexpressing hypertensive mice[J]. European Heart Journal, 2018, 39(suppl_1): ehy564. P938.
FSLLRY-NH2是蛋白酶激活受体2（PAR-2）的拮抗剂 [1]。FSLLRY-NH2通过结合PAR-2的外环2（ECL-2）区域抑制受体活化，从而阻断蛋白酶诱导的信号转导 [2]。FSLLRY-NH2应用于炎症、瘙痒和免疫反应的研究 [3-4]。
在HepG2细胞中，FSLLRY-NH2（100-300μM；24h）通过SAPK/JNK通路降低H2O2诱导的促炎基因IL-8、IL-1β和TNF-α的水平 [5]。在A549细胞中，FSLLRY-NH2（100μM；24h）抑制细胞中PAR2的表达 [6]。
在窒息性心脏骤停（ACA）诱发的大鼠模型中，FSLLRY-NH2（50µg；鼻腔给药；单次给药）治疗显著改善了神经系统预后，并减少了ACA后退化的海马神经元数量 [7]。在Ren-TG小鼠中，FSLLRY-NH2（10μg/kg；sc；4周）治疗减弱了PAR-2、β-MHC、COL3A1和 TGF-β1等心脏总mRNA表达的增加 [8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells grown in a six-well plate were stimulated with hydrogen peroxide (100, 200, 300, 400, 600μM) and FSLLRY-NH2 (100, 150, 200, 250, 300μM) for 24h and cell lysates prepared. Equal amounts of protein from each lysate were then separated by electrophoresis on SDS polyacrylamide gels (10–14%). Proteins were then transferred to an NC membrane using a Power Pac 1000 power supply. To block any nonspecific binding, the nitrocellulose (NC) membrane was incubated in 5% nonfat dry milk, or in TBST, for greater than 60min, followed by four rinses in milk-free TBST. The membranes were incubated overnight at 4℃ with shaking with primary antibodies raised against PAR2, IL 1b, IL-8, TNF-a, and SAPK/JNK, followed by four washes with TBS containing 0.1% Tween 20. This was followed by 90min incubation in horseradish peroxidase-conjugated secondary antibody. Immuno-reactive proteins were detected using the ECL reagent. Molecular masses were estimated by comparison with a pre-stained molecular mass marker. To confirm the uniformity of protein loading, the same blots were subsequently stripped with western blot stripping buffer and re-probed with an anti-actin antibody. The results were analyzed using Quantity One analysis software. The percent of PAR2 expression or IL-1b, IL-8, TNF-a, SAPK/JNK expression were calculated against control bands. |
Reaction Conditions | 100-300μM; 24h |
Applications | FSLLRY-NH2 reduces the level of the pro-inflammatory genes IL-8, IL-1b, and TNF-α induced by H2O2, through the SAPK/JNK pathways in HepG2 cells. |
| Animal experiment [2]: | |
Animal models | Asphyxial cardiac arrest (ACA)-induced rat model |
Preparation Method | One hour after ACA, FSLLRY-NH2 was diluted in 20% ethanol and administered intranasally. Briefly, the animals were placed in supine position under 2% isoflurane anesthesia. A total volume of 30 microliters (μL) of vehicle (20% ethanol) or FSLLRY-NH2 (50µg/rat) in 20% ethanol was administered to the left and right nares, alternately administering 5μL in one naris every 2 minutes for a period of 10 minutes. |
Dosage form | 50µg; nas; single administration |
Applications | FSLLRY-NH2 treatment significantly improved neurological outcomes and reduced the number of degenerating hippocampal neurons after ACA. |
References: | |
| Cas No. | 245329-02-6 | SDF | |
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CC=CC=C1)([H])CO)([H])CC(C)C)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC2=CC=C(O)C=C2)([H])CCCNC(N)=N)C | ||
| 分子式 | C39H60N10O8 | 分子量 | 796.97 |
| 溶解度 | ≥ 26.9mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2548 mL | 6.2738 mL | 12.5475 mL |
| 5 mM | 251 μL | 1.2548 mL | 2.5095 mL |
| 10 mM | 125.5 μL | 627.4 μL | 1.2548 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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