13390  N-methyl Leukotriene C4

N-methyl LTC4 (CAS 131391-65-6)

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.2 LTC4, 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
1  J. A. Maclouf and R. C. Murphy. 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  P. J. Piper. Formation and actions of leukotrienes. Physiological Reviews 64 744-761 (1984).
3  B. J. Campbell, S. F. Baker, S. D. Shukla, et al. Bioconversion of leukotriene D4 by lung dipeptidase. Biochimica et Biophysica Acta 1042 107-112 (1990).
4  Y. Gareau, R. Zamboni and A. W. Wong. Total synthesis of N-methyl LTC4: A novel methodology for the monomethylation of amines. The Journal of Organic Chemistry 58 1582-1585 (1993).
5  D. Yan, R. Stocco, N. Sawyer, 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).

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25 µg €168.00
50 µg €319.00
100 µg €603.00
Pricing updated 2017-01-19.
Prices are subject to change without notice.