货号 | 10007565-100mg |
描述 | Lysophosphatidic acid (LPA) is a lipid signalling molecule formed by the hydrolysis of lysophosphatidyl choline by lysophospholipase D, also known as autotaxin (ATX).1 LPA signals through four different G protein-coupled receptors, LPA1/EDG-2, LPA2/EDG-4, LPA3/EDG-7, and LPA4/GPR23.2,3 Activation of peroxisome proliferator-activated receptor γ (PPARγ) by LPA has also been reported.4 Tetradecyl phosphonate is a pan-antagonist of lysophosphatidic acid 1 (LPA1), LPA2, and LPA3 receptors with IC50 values for inhibition of LPA-induced calcium mobilization of 10 µM, 5.5 µM, and 3.1 µM, respectively.5 At a concentration of 10 µM, tetradecyl phosphonate activates a peroxisome proliferator-activated receptor γ reporter construct 4-fold compared to controls and partially inhibits autotaxin with an IC50 of approximately 3 µM.5 |
供应商 | Cayman |
应用文献 | |
1.Tokumura, A.,Majima, E.,Kariya, Y., et al. Identification of human lysophospholipase D, a lysophosphatidic acid-producing enzyme, as autotaxin, a multifunctional phosphodiesterase. The Journal of Biological Chemisty 277(42), 39436-39442 (2002). 2.Chun, J.,Goetzl, E.J.,Hla, T., et al. International union of pharmacology. XXXIV. Lysophospholipid receptor nomenclature. Pharmacological Reviews 54, 265-269 (2002). 3.Noguchi, K.,Ishii, S., and Shimizu, T. Identification of p2y9/GPR23 as a novel G protein-coupled receptor for lysophosphatidic acid, structurally distant from the Edg family. The Journal of Biological Chemisty 278(28), 25600-25606 (2003). 4.McIntyre, T.M.,Pontsler, A.V.,Silva, A.R., et al. Identification of an intracellular receptor for lysophosphatidic acid (LPA): LPA is a transcellular PPARγ agonist. Proceedings of the National Academy of Sciences of the United States of America 100(1), 131-136 (2003). 5.Durgam, G.G.,Virag, T.,Walker, M.D., et al. Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptors ligands, activators of PPARγ, and inhibitors of autotaxin. Journal of Medicinal Chemistry 48, 4919-4930 (2005). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 278.4 |
分子式 | C14H31O3P |
CAS号 | 4671-75-4 |
稳定性 | ≥ 2 years |
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