CAY10444 (Synonyms: BML-241) |
| Catalog No.GC18757 |
CAY10444 (BML-241) es un antagonista de la esfingosina-1-fosfato 3 (S1P3). CAY10444 inhibe en un 37 % los aumentos inducidos por S1P en Ca2+ en células HeLa que expresan receptores S1P3.
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Cas No.: 298186-80-8
Sample solution is provided at 25 µL, 10mM.
A family of related G-protein coupled receptors that bind sphingosine-1 phosphate (S1P) as a high-affinity ligand have recently been cloned.[1],[2] S1P3/EDG3 is a member of this family that is widely expressed in many tissues, signaling via the ERK-½ and PLC/IP3 pathways. CAY10444 is a selective antagonist of S1P binding to the S1P3 receptor, blocking the calcium increase in HeLa cells by about 40% when present at 10 µM.[3]
Reference:
[1]. Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim. Biophys. Acta 1582(1-3), 72-80 (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]. Koide, Y., Hasegawa, T., Takahashi, A., et al. Development of novel EDG3 antagonists using a 3D database search and their structure-activity relationships. Journal of Medicinal Chemistry 45, 4629-4638 (2002).
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