CAY10650
目录号 : GC18305
CAY10650是一种高效的细胞质磷脂酶A2α（cPLA2α）抑制剂，IC50值为12nM。
Cas No.:1233706-88-1
Sample solution is provided at 25 µL, 10mM.
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CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12nM[1]. cPLA2α is a crucial enzyme involved in the hydrolysis of phospholipids to release arachidonic acid and is essential for mediating inflammatory responses and cellular signaling pathways[2][3]. CAY10650 is typically used for studying inflammation and cellular signaling pathways related to phospholipase A2[4][5].
In vitro, CAY10650 (12nM; 30min) inhibit the phosphorylation of cPLA2α, and reduced lipid body formation and PGE2 secretion in human neutrophils stimulated with Cr-LAAO[1].
In vivo, CAY10650 (50μg in 5μl eye-drop) attenuated corneal inflammation and decreased neutrophil infiltration when applied topically three times daily for 6 days and then daily from days 7 to 15 post-infection in Chinese hamsters infected with Acanthamoeba castellanii in the eyes[6]. CAY10650 (20μg/ear/day) reduced ear thickness, epidermal thickness, and inflammatory infiltrates in an IMQ-induced psoriasis mouse model when applied topically for 5 days[7].
References:
[1] Paloschi MV, Lopes JA, Boeno CN, et al. Cytosolic phospholipase A2-α participates in lipid body formation and PGE2 release in human neutrophils stimulated with an L-amino acid oxidase from Calloselasma rhodostoma venom. Sci Rep. 2020;10(1):10976.
[2] Murakami M, Kudo I. Phospholipase A2. J Biochem. 2002;131(3):285-292.
[3] Yang D, Ji HF, Zhang XM, et al. Protective effect of cytosolic phospholipase A2 inhibition against inflammation and degeneration by promoting regulatory T cells in rats with experimental autoimmune encephalomyelitis. Mediators Inflamm. 2014;2014:890139.
[4] Lin CY, Xu WB, Li BZ, Shu MA, Zhang YM. Identification and functional analysis of cytosolic phospholipase A2 (cPLA2) from the red swamp crayfish Procambarus clarkii: The first evidence of cPLA2 involved in immunity in invertebrates. Fish Shellfish Immunol. 2023;140:108944.
[5] Wu CZ, Li X, Hong L, et al. NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria. Korean J Physiol Pharmacol. 2021;25(2):159-166.
[6] Tripathi T, Abdi M, Alizadeh H. Role of phospholipase A₂ (PLA₂) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013;113:182-191.
[7] Shao S, Chen J, Swindell WR, et al. Phospholipase A2 enzymes represent a shared pathogenic pathway in psoriasis and pityriasis rubra pilaris. JCI Insight. 2021;6(20):e151911.
CAY10650是一种高效的细胞质磷脂酶A2α（cPLA2α）抑制剂，IC50值为12nM[1]。cPLA2α是一种关键酶，参与磷脂的水解以释放花生四烯酸，对于介导炎症反应和细胞信号传导通路至关重要[2][3]。CAY10650通常用于研究与磷脂酶A2相关的炎症和细胞信号传导通路研究[4][5]。
在体外实验中，CAY10650（12nM；30分钟）抑制了Cr-LAAO刺激的人类中性粒细胞中cPLA2α的磷酸化，并减少了脂滴形成和PGE2分泌[1]。
在体内实验中，CAY10650（50μg in 5μl眼药水）通过局部给药，每天三次，持续6天，然后从第7天到第15天每天一次，用于眼部感染棘阿米巴原虫的中国仓鼠，显著减轻了角膜炎症并减少了中性粒细胞的浸润[6]。CAY10650（20μg/耳/天）在IMQ诱导的银屑病小鼠模型中，通过局部给药，连续5天，显著减少了耳部厚度、表皮厚度和炎症细胞浸润[7]。
| Cell experiment [1]: | |
Cell lines | human neutrophils |
Preparation Method | Neutrophils isolated according to item above from 3 different donors, were suspended in a RPMI assay medium [RPMI-1640 medium supplemented with 100mg/mL of gentamicin, 2mM of l-glutamine and 2% of fetal bovine serum (FBS)]. 1×107 isolated human neutrophils were plated and pre-treated with CAY10650 (cPLA2-α inhibitor, 12nM for 30min) or the same vehicle used to dissolve the inhibitors in RPMI (control). Then, they were incubated with RPMI (negative control), LPS (1µg/mL; positive control) or Cr-LAAO (50µg/mL) at 37°C, in a humidified atmosphere (5% CO2) for 1h. Lipid bodies were quantified with Oil Red O staining. PGE2 concentrations in the supernatant were determined by a specific enzymatic immunoassay (EIA). Proteins were extracted for western blot analysis. |
Reaction Conditions | 12nM; 30min |
Applications | CAY10650 inhibit the phosphorylation of cPLA2α, and reduced lipid body formation and PGE2 secretion in human neutrophils stimulated with Cr-LAAO. |
| Animal experiment [2]: | |
Animal models | Chinese hamsters |
Preparation Method | Chinese hamsters (n=9/group) were infected with Acanthamoeba castellanii-laden contact lenses. cPLA2α inhibitor (CAY10650; 50μg in 5μl) was injected with topical eye-drop under the contact lens of an infected cornea three times a day for 6 days and topically on days 7 to 20 postinfection. As a control infected animals were treated with 50μg/5μl of BSA. Lenses were removed 7 days postinfection, and corneas were scored for clinical severity for the period indicated. Each graph line represents the mean severity of the observed time points. The results shown are representative of three separate experiments. The infections were scored on a scale of 0 to 5 based on the following parameters: corneal infiltration, corneal neovascularization and corneal ulceration. The pathology was recorded as: 0=no pathology, 1=<10% of the cornea involved, 2=10 to 25% involved, 3=25 to 50% involved, 4=50 to 75% involved, and 5=75 to 100% involved. Any animals receiving a score of at least 1.0 for any parameter were scored as infected. Animals were anesthetized and sacrificed 15 days after application of CAY10650. Each animal’s right eye (uninfected and untreated) was used as negative control. As control, uninfected eyes of animals (n=6/group) were treated with CAY10650. Eyes were removed and used for histopathological examination. |
Dosage form | 50μg in 5μl eye-drop; topically three times daily for 6 days and then daily from days 7 to 15 post-infection |
Applications | CAY10650 attenuated corneal inflammation and decreased neutrophil infiltration when applied topically three times daily for 6 days and then daily from days 7 to 15 post-infection in Chinese hamsters infected with Acanthamoeba castellanii in the eyes. |
References: | |
| Cas No. | 1233706-88-1 | SDF | |
| 化学名 | 3-(2-methyl-1-oxopropyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid | ||
| Canonical SMILES | O=C(CN1C(C=CC(C(O)=O)=C2)=C2C(C(C(C)C)=O)=C1)COC3=CC=C(OC4=CC=CC=C4)C=C3 | ||
| 分子式 | C28H25NO6 | 分子量 | 471.5 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1209 mL | 10.6045 mL | 21.2089 mL |
| 5 mM | 424.2 μL | 2.1209 mL | 4.2418 mL |
| 10 mM | 212.1 μL | 1.0604 mL | 2.1209 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。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet