货号 | 13390-100ug |
描述 | Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4(LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4.1 It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity.2LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult.3 N-methyl Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4.4It acts as a potent and selective CysLT2 receptor agonist exhibiting EC50 values of 122 and > 2,000 nM at the human CysLT2 and CysLT1 receptors, respectively.5 It has essentially the same potency as LTC4 at both the human and murine receptors CysLT2 receptors. N-methyl LTC4 is potent and active in vivo, causing vascular leak in mice overexpressing the human CysLT2 receptor but not in CysLT2 receptor knockout mice.5 |
别名 | N-methyl LTC4; |
供应商 | Cayman |
应用文献 | |
1.Maclouf, J.A., and Murphy, R.C. Transcellular metabolism of neutrophil-derived leukotriene A4 by human platelets. A potential cellular source of leukotriene C4. The Journal of Biological Chemisty 263, 174-181 (1988). 2.Piper, P.J. Formation and actions of leukotrienes. Physiological Reviews 64, 744-761 (1984). 3.Campbell, B.J.,Baker, S.F.,Shukla, S.D., et al. Bioconversion of leukotriene D4 by lung dipeptidase. Biochimica et Biophysica Acta 1042, 107-112 (1990). 4.Gareau, Y.,Zamboni, R., and Wong, A.W. Total synthesis of N-methyl LTC4: A novel methodology for the monomethylation of amines. The Journal of Organic Chemistry 58, 1582-1585 (1993). 5.Yan, D.,Stocco, R.,Sawyer, N., et al. Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT2) agonist, N-methyl-leukotriene C4, in calcium reporter andβarrestin assays. Molecular Pharmacology (2010). | |
运输条件 | Dry ice in continental US; may vary elsewhere |
存放说明 | -80 |
纯度 | ≥97% |
计算分子量 | 639.8 |
分子式 | C31H49N3O9S |
CAS号 | 131391-65-6 |
稳定性 | ≥ 1 year |
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