LPA2 antagonist 1
(Synonyms: LPA2-IN-1) 目录号 : GC12655LPA2 antagonist 1是一种LPA2拮抗剂，其IC50值为17nM。
Cas No.:1017606-66-4
Sample solution is provided at 25 µL, 10mM.
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LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17nM[1]. LPA2 (Lysophosphatidic Acid Receptor 2), also known as EDG4, is a G-protein coupled receptor that mediates various cellular responses such as cell adhesion, migration, and proliferation after activated by lysophosphatidic acid (LPA)[2]. LPA2 antagonist 1 is usually used in research related to inflammation and cancer [3][4].
In vitro, pretreatment of cortical neurons with LPA2 antagonist 1 (0.05µM; 2h) significantly reduced neuronal apoptosis induced by LPA treatment[5]. Pretreatment of IEC-6 cells with LPA2 antagonist 1 (0.2µM or 1µM; 30min prior to LPA treatment) significantly increased the percentage of γ-H2AX-positive cells after irradiation[6].
In vivo, LPA2 antagonist 1 (5mg/kg; i.p.; 10min pretreatment) decreased circulating GLP-1 concentrations in C57BL/6J mice but failed to significantly reverse the LPA-induced suppression of GLP-1 levels in vivo[7].
References:
[1] Beck HP, Kohn T, Rubenstein S, et al. Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg Med Chem Lett. 2008;18(3):1037-1041.
[2] Huang MC, Graeler M, Shankar G, Spencer J, Goetzl EJ. Lysophospholipid mediators of immunity and neoplasia. Biochim Biophys Acta. 2002;1582(1-3):161-167.
[3] Balijepalli P, Sitton CC, Meier KE. Lysophosphatidic Acid Signaling in Cancer Cells: What Makes LPA So Special?. Cells. 2021;10(8):2059.
[4] Yung YC, Stoddard NC, Chun J. LPA receptor signaling: pharmacology, physiology, and pathophysiology. J Lipid Res. 2014;55(7):1192-1214.
[5] Wang Y, Zhang J, Huang L, et al. The LPA-CDK5-tau pathway mediates neuronal injury in an in vitro model of ischemia-reperfusion insult. BMC Neurol. 2022;22(1):166.
[6] Balogh A, Shimizu Y, Lee SC, et al. The autotaxin-LPA2 GPCR axis is modulated by γ-irradiation and facilitates DNA damage repair. Cell Signal. 2015;27(9):1751-1762.
[7] Fernandes MF, Tomczewski MV, Duncan RE. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid. Int J Mol Sci. 2022;23(8):4163.
LPA2 antagonist 1是一种LPA2拮抗剂，其IC50值为17nM[1]。LPA2（溶血磷脂酸受体2），也被称为EDG4，是一种G蛋白偶联受体，被溶血磷脂酸（LPA）激活时，可介导多种细胞反应，如细胞粘附、迁移和增殖[2]。LPA2 antagonist 1通常用于与炎症和肿瘤相关的研究[3][4]。
在体外实验中，用LPA2 antagonist 1（0.05µM；2小时）预处理皮质神经元可显著减少LPA处理诱导的神经元凋亡[5]。用LPA2 antagonist 1（0.2µM或1µM；LPA处理前30分钟）预处理IEC-6细胞可显著增加辐射后γ-H2AX阳性细胞的百分比[6]。
在体内实验中，LPA2 antagonist 1（5mg/kg；腹腔注射；10分钟预处理）可降低C57BL/6J小鼠的循环GLP-1浓度，但未能显著逆转LPA诱导的体内GLP-1水平抑制[7]。
| Cell experiment [1]: | |
Cell lines | IEC-6 cells |
Preparation Method | IEC-6 cells were grown in complete medium supplemented with 10μg/ml insulin. Prior to 15Gy γ-radiation, cells were serum starved overnight and treated with 10μM LPA or vehicle (0.1% BSA). After irradiation, the medium was replaced with serum-free medium containing either LPA or vehicle. At the indicated time points (0.5, 1, 2, 4, 6, 8 hours post radiation), cells were trypsinized, washed with cold PBS and stained with anti-human/mouse phospho-H2AX labeled with eFluor660. For inhibition of the LPA2 receptor, the cells were treated with 0.2μM or 1μM of the LPA2 antagonist 1 for 30min followed by 15min of 10μM LPA treatment prior to irradiation. After irradiation, the culture medium was changed to fresh medium containing the antagonist and LPA. Cells were harvested and stained for γ-H2AX 6h after irradiation. Fluorescence was measured using a LSR II instrument and analyzed with the FACSDiva software. |
Reaction Conditions | 0.2µM or 1µM; 30min prior to LPA treatment |
Applications | Pretreatment of IEC-6 cells with LPA2 antagonist 1 significantly increased the percentage of γ-H2AX-positive cells after irradiation. |
| Animal experiment [2]: | |
Animal models | C57BL/6J male mice |
Preparation Method | Experiments were performed in 16-18-week-old C57BL/6J male mice, housed in a temperature- and humidity-controlled environment on a 12:12h light/dark cycle. At timepoint 0, mice were injected i.p. with vehicle control (10% DMSO) or LPA2 antagonist 1 (5mg/kg). Ten minutes later, mice were injected i.p. with vehicle control (isotonic saline) or 18:1-LPA (50mg/kg). Thirty minutes later, mice were euthanized by cervical dislocation and whole blood was rapidly collected by cardiac puncture. Blood was allowed to clot and centrifuged at 1000×g for 10min in a refrigerated centrifuge. Serum was collected and stored at -20℃ until assay for GLP-1 secretion using a GLP-1 EIA Kit. |
Dosage form | 5mg/kg; i.p.; 10min pretreatment |
Applications | LPA2 antagonist 1 decreased circulating GLP-1 concentrations in C57BL/6J mice and failed to significantly reverse the LPA-induced suppression of GLP-1 levels in vivo. |
References: | |
| Cas No. | 1017606-66-4 | SDF | |
| 别名 | LPA2-IN-1 | ||
| 化学名 | (S)-N-(1-(4-((3,4-dichlorophenyl)sulfonyl)piperazin-1-yl)propan-2-yl)-7-methylthieno[3,2-d]pyrimidin-4-amine | ||
| Canonical SMILES | CC1=CSC2=C1N=CN=C2N[C@@](CN3CCN(S(C4=CC(Cl)=C(Cl)C=C4)(=O)=O)CC3)([H])C | ||
| 分子式 | C20H23Cl2N5O2S2 | 分子量 | 500.46 |
| 溶解度 | ≥ 19.1mg/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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9982 mL | 9.9908 mL | 19.9816 mL |
| 5 mM | 399.6 μL | 1.9982 mL | 3.9963 mL |
| 10 mM | 199.8 μL | 999.1 μL | 1.9982 mL |
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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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工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >99.50%
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