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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
1
Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim Biophys Acta158272-80(2002).
2
Chun, J., Goetzl, E.J., Hla, T., et al. International union of pharmacology. XXXIV. Lysophospholipid receptor nomenclature. Pharmacol Rev54265-269(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. J Med Chem454629-4638(2002).
Synonyms
BML-241
Formal Name
2-undecyl-thiazolidine-4-carboxylic acid
CAS Number
298186-80-8
Molecular Formula
C15H29NO2S
Formula Weight
287.5
Formulation
A crystalline solid
Purity
≥98%
Stability
1 year
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
[H]N1C(CCCCCCCCCCC)SC[C@H]1C(O)=O
Background Reading
Chun, J., Goetzl, E.J., Hla, T., et al. International union of pharmacology. XXXIV. Lysophospholipid receptor nomenclature. Pharmacol Rev54265-269(2002).
Koide, Y., Hasegawa, T., Takahashi, A., et al. Development of novel EDG3 antagonists using a 3D database search and their structure-activity relationships. J Med Chem454629-4638(2002).
Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim Biophys Acta158272-80(2002).
CAY10444 is available in the following screening
library: