Cat. No. | Product Name | Target | Signaling Pathways |
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T21654 |
1-Oleoyl lysophosphatidic acid sodium
1-Oleoyl lysophosphatidic acid sodium salt |
LPA Receptor | GPCR/G Protein |
1-Oleoyl lysophosphatidic acid sodium (1-Oleoyl lysophosphatidic acid sodium salt) salt 是 LPA1 和 LPA2 的内源性激动剂,可通过诱导 DNA 合成促进有丝分裂,参与正常和病理性情绪反应,如焦虑和抑郁。 | |||
T36907 |
1-Oleoyl Lysophosphatidic Acid
Oleoyl-sn-3-Glycerophosphate,1-Oleoyl LPA,1-Oleoyl Lysophosphatidic Acid |
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1-Oleoyl lysophosphatidic acid is a species of lysophosphatidic acid (LPA) containing oleic acid at the sn-1 position. Phosphatidic acid is produced either directly through the action of phospholipase D (PLD) or through a two step process involving liberation of diacylglycerol (DAG) by phospholipase C (PLC) followed by phosphorylation of DAG by diglycerol kinase.[1] Hydrolysis of the fatty acid at the sn-2 position by phospholipase A2 (PLA2) yields bioactive LPA. LPA binds to one of five differe... | |||
T83879 |
1-Arachidoyl Lysophosphatidic Acid sodium
1-Arachidoyl LPA,LPA(20:0),1-Eicosanoyl-Lysophosphatidic Acid |
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1-花生四烯酰基溶血磷脂酸(1-arachidoyl LPA)是溶血磷脂酸受体1(LPA1)的激动剂,并且是一种含有花生四烯酸的甘油磷脂,花生四烯酸位于sn-1位置。它能在主要表达LPA1而非LPA2-LPA6的人类肺成纤维细胞中诱导钙离子动员(EC50 = 3.6 µM)。在无细胞试验中,1-Arachidoyl LPA(2.5 µM)还能结合到过氧化物酶体增殖物激活受体γ(PPARγ)的配体结合域。人类尿液中也发现了该化合物。 | |||
T36768 |
1-Octadecyl Lysophosphatidic Acid
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1-Octadecyl lysophosphatidic acid (1-octadecyl LPA) is a LPA analog containing stearic acid at the sn-1 position. LPA binds to one of five different G protein linked receptors to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility. Alkyl ether-linked LPA derivatives have a higher platelet aggregating activity than the acyl derivatives, most likely stemming from an alkyl-specific LPA recepto... | |||
T33076 |
Lysophosphatidic acid
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Lysophosphatidic acid is a bioactive chemical. | |||
T36452 |
1-Arachidonoyl Lysophosphatidic Acid (ammonium salt)
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1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differe... | |||
T37283 |
1-Palmitoyl Lysophosphatidic Acid (sodium salt)
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1-Palmitoyl lysophosphatidic acid (1-Palmitoyl LPA) is a LPA analog containing palmitic acid at the sn-1 position. LPA binds to one of five different G protein-coupled receptors (GPCRs) to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility. In addition to playing a role in the aforementioned biological responses, 1-palmitoyl LPA enhances the action of β-lactam antibiotics (ampicillin, pipe... | |||
T37282 |
1-Palmitoyl Lysophosphatidic Acid
|
Antibacterial | Microbiology/Virology |
1-Palmitoyl Lysophosphatidic Acid 是 LPA 的类似物,通过结合 Ca2+ 和 Mg2+ 提高氨苄西林、哌拉西林和头孢他啶对各种铜绿假单胞菌菌株的作用。 | |||
T77789 |
Oleoyl-L-alpha-lysophosphatidic acid sodium salt
LPA sodium salt |
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Oleoyl-L-alpha-lysophosphatidic acid sodium salt为必需的细胞膜生物合成代谢物,可通过与G蛋白偶联受体(GPCR)(即LPA受体)相互作用来介导信号传导,是LPA1和LPA2受体的内源性激动剂。 | |||
T83772 |
1-Linoleoyl Lysophosphatidic Acid sodium
1-Linoleoyl-2-hydroxy-sn-glycero-3-PA,LPA(18:2),PA(18:2(9Z,12Z)/0:0),1-Octadecadienoyl-2-hydroxy-sn-glycero-3-phosphate,18:2 Lyso PA,1-Octadecadienoyl-2-hydroxy-sn-glycero-3-PA,PA(18:2/0:0),1-Linoleoyl-2-hydroxy-sn-glycero-3-phosphate,1-Linoleoyl LPA |
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1-Linoleoyl LPA(1-亚油酰LPA)是LPA2受体的激动剂,属于一种含有亚油酸的甘油磷脂,在sn-1位置含亚油酸。它是小鼠和人体血浆中最丰富的LPA。1-Linoleoyl LPA在表达LPA2受体的Sf9细胞中选择性地增加细胞内钙水平(EC50约为10 nM),相较于表达LPA1和LPA3受体的Sf9细胞(EC50分别约为200和80 nM)。携带NCTC克隆2472肿瘤的小鼠中,1-linoleoyl LPA的血清水平增加。与患有初发进行性多发性硬化症的患者相比,复发缓解型多发性硬化症患者的血浆1-Linoleoyl LPA水平降低,且与神经功能缺损严重程度负相关。 | |||
T22834 |
H2L 5765834
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LPA Receptor; LPL Receptor | GPCR/G Protein |
H2L 5765834 是溶血磷脂酸受体 LPA1、LPA3和 LPA5拮抗剂,IC50值分别为 94、752 和 463 nM。 | |||
T11533 |
Z-HA155
CS-963 |
PDE | Metabolism |
Z-HA155 (CS-963) 是一种高效的 ATX 选择性抑制剂,其 IC50=5.7 nM。 | |||
T21694 |
(R)-Lisofylline
(R)-Lisophylline |
STAT | JAK/STAT signaling; Stem Cells |
(R)-Lisofylline ((R)-Lisophylline) 是溶血磷脂酸酰基转移酶的抑制剂 (IC50 = 0.6 µM)。 (R)-Lisofylline 可中断 IL-12 信号介导的 STAT4 激活,可用于治疗 1 型糖尿病和自身免疫性疾病的研究。 | |||
T2008 |
LY294002
LY 294002,NSC 697286,SF 1101 |
Apoptosis; DNA-PK; Casein Kinase; PI3K; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
LY294002 (SF 1101) 是一种 PI3K 的广谱抑制剂,抑制 PI3Kα、PI3Kδ 和 PI3Kβ (IC50=0.5/0.57/0.97 μM)。LY294002 也是 DNA-PK 抑制剂 (IC50=1.4 μM) 和 CK2 抑制剂 (IC50=98 nM)。LY294002 可以激活凋亡和自噬。 | |||
T4079 |
LY-294002 hydrochloride
SF 1101,LY 294002,NSC 697286 |
PI3K | PI3K/Akt/mTOR signaling |
LY-294002 hydrochloride (NSC 697286) 是一种合成的 PI3Kα/δ/β 分子抑制剂(IC50:0.5/0.57/0.97 μM,在无细胞试验中);在溶液中比 Wortmannin 更稳定,也是自噬体形成的阻断剂。 | |||
T7689 |
Tetradecyl Phosphonate
|
LPA Receptor | GPCR/G Protein |
Tetradecyl Phosphonate 是溶血磷脂酸 1 (LPA1)、LPA2 和 LPA3 受体的泛拮抗剂。 | |||
T7393 |
ONO-7300243
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LPA Receptor; LPL Receptor | GPCR/G Protein |
ONO-7300243 是溶血磷脂酸受体 1 (LPA1)拮抗剂,IC50为 0.16 μM。 | |||
T15785 |
LPA1 receptor antagonist 1
LPA1 R antagonist 1 |
LPA Receptor | GPCR/G Protein |
LPA1 receptor antagonist 1(LPA1 R antagonist 1) 是一种具有选择性和高效性的溶血磷脂酸 (LPA1) 受体拮抗剂( IC50 : 25 nM),可用于研究特发性肺纤维化。 | |||
T10415 |
Autotaxin-IN-3
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PDE | Metabolism |
Autotaxin-IN-3 是 Autotaxin 的抑制剂(IC50 = 2.4 nM),Autotaxin 负责增加腹水和血浆中的溶血磷脂酸。 | |||
T10381 |
AS2717638
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Others | Others |
AS2717638 是一种具有口服生物活性的,选择性的溶血磷脂酸受体5 (LPA5) 的拮抗剂,其对 hLPA4 的 IC50值为38 nM。AS2717638 还能显著改善 PGE2、PGF2α以及 AMPA 诱导的异位疼痛。 | |||
T3631 |
PF-8380
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PDE | Metabolism |
PF8380 是有效的autotaxin 抑制剂,在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。 | |||
T22070 |
DBIBB
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LPA Receptor | GPCR/G Protein |
DBIBB 是一种特异性溶血磷脂酸 (LPA2) 的 2 型 G 蛋白偶联受体的非脂质激动剂,是一种能够治疗高强度γ 射线对造血和胃肠系统引起的急性放射综合征的潜在活性分子 ,是一种作未有机合成和药物研究中的中间体。 DBIBB 可用于制备各种化合物,可减轻胃肠道辐射综合征,增加肠隐窝存活率和肠细胞增殖,并减少细胞凋亡 。 | |||
T25847 |
NAEPA
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NAEPA, an LPA mimetic, is a selective agonist of the lysophosphatidic acid-1 (LPA1) receptor. | |||
T29109 |
VPC12249
VPC-12249,VPC 12249 |
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VPC12249, a lysophosphatidic acid receptor type 1 (LPA1) antagonist, plays a functional role in osteoclast differentiation and bone resorption activity. | |||
T63645 |
ONO-9780307
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ONO-9780307 是 LPA1 (lysophosphatidic acid receptor 1) 的特异性拮抗剂 (IC50: 2.7 nM)。 | |||
T14335 | ASP6432 | LPA Receptor | GPCR/G Protein |
ASP6432 is an antagonist of type 1 lysophosphatidic acid receptor (LPA1). For human LPA1 and rat LPA1, the IC50s are 11 nM and 30 nM , respectively. | |||
T28300 |
PAT-347 sodium
PAT-347,PAT347,PAT 347 |
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PAT-347 is a potent inhibitor of Autotaxin (ATX), a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. | |||
T73017 |
ONO-0740556
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ONO-0740556 是一种有效的 Gi 偶联人类溶血磷脂酸受体1 (LPA1) 激动剂,其EC50值为 0.26 nM。 | |||
T69647 |
UCM-05194
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UCM-05194 is a potent Agonist of the Type 1 Lysophosphatidic Acid Receptor (LPA1). UCM-05194 Shows Efficacy in Neuropathic Pain Amelioration. UCM-05194 stands out as the most potent and selective LPA1 receptor agonist described so far (Emax = 118%, EC50 = 0.24 μM, KD = 19.6 nM; inactive at autotaxin and LPA2-6 receptors). | |||
T16434 |
PAT-048
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PDE | Metabolism |
PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. | |||
T83882 |
XY-4
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XY-4是1-棕榈酰基溶血磷脂酸(1-palmitoyl LPA094)的衍生物,同时也是过氧化物酶体增殖物激活受体γ(PPARγ)的激动剂。当浓度为5 µM时,能在表达过氧化物酶体增殖物反应元件(PPRE)的RAW 264.7巨噬细胞中诱导报告基因的表达。XY-4不作为溶血磷脂酸受体1(LPA1)、LPA2或LPA3的激动剂。在1 µM的浓度下,它能在体外诱导血小板聚集。XY-4诱导大鼠颈动脉内膜新生。 | |||
T63231 | LPA5 antagonist 1 | ||
LPA5 antagonist 1 是选择性的、强效的 lysophosphatidic acid receptor 5(LPA5) 拮抗剂,IC50 值为32 nM。LPA5 antagonist 1 具有高脑渗透性和抗痛活性,能够用于研究炎症性和神经性疼痛。 | |||
T27094 |
CT-2584
CT2584 |
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CT-2584 is an angiogenesis inhibitor and lysophosphatidic acid acyltransferase inhibitor. CT-2584 inhibits phospholipid signaling. By inhibiting CTP:choline-phosphate cytidylyltransferase (CT), CT-2584 caused de novo phospholipid biosynthesis via PA to be | |||
T70275 |
PAT-347
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PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others. | |||
T36138 |
BMP-22
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BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngene... | |||
T63439 | BMS-986020 sodium | ||
BMS-986020 sodium 是高亲和力的溶血磷脂酸受体 1 (LPA1) 拮抗剂,能够抑制胆汁酸和磷脂转运蛋白,并抑制 BSEP (IC50: 4.8 μM),MRP4 (IC50: 6.2 μM) 和 MDR3 (IC50: 7.5 μM)。BMS-986020 sodium 表现出特发性肺纤维化 (IPF) 的研究潜力。 | |||
T37691 |
Phosphatidic Acids (egg) (ammonium salt)
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Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular ... | |||
T36502 |
DCP-Rho1
DCP-Rho1 |
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DCP-Rho1 is a fluorescent probe for the detection of sulfenic acid-containing proteins.1,2 It displays excitation/emission maxima of 560/581 nm, respectively, and has been used to visualize protein oxidation sites in situ. |1. Klomsiri, C., Rogers, L.C., Soito, L., et al. Endosomal H2O2 production leads to localized cysteine sulfenic acid formation on proteins during lysophosphatidic acid-mediated cell signaling. Free Rad. Biol. Med. 71, 49-60 (2014).|2. Holmila, R.J., Vance, S.A., Chen, X., et ... |