Cayman 1-Stearoyl-Rac-Glycerol; Purity- Greater Than Or Equal To

The prostaglandin E₂ (PGE₂) receptor EP₁ is involved in triggering PGE₂-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE₂ at the EP₁ receptor.^, At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE₂-induced smooth muscle contractions of guinea pig ileum and stomach.^, SC-19220 also acts as a PGE₂ antagonist in the EP₁ receptor-mediated contraction of guinea pig trachea. SC-19220 displaces radiolabeled PGE₂ from the cloned human EP₁ receptor with an IC₅₀ of 6.7 µM and exhibits no binding at the human EP₂ receptor.^, It binds with apparent low affinity to the cloned mouse EP₁ receptor expressed in CHO cells. In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D₃- and PGE₂-stimulated osteoclastogenesis in mouse osteoclast precursors. Antagonism of EP₁ with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer. In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE₂-mediated loss of dopaminergic neurons from rat substantia nigra.

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