10011561  SC-51089

CID132748 (CAS 146033-02-5)

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The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat.1,2 SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo.3 In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.4,5
1  Hallinan, E.A., Hagen, T.J., Husa, R.K., et al. N-substituted dibenzoxazepines as analgesic PGE2 antagonists. J Med Chem 36 3293-3299 (1993).
2  Malmberg, A.B., Rafferty, M.F., Yaksh, T.L. Antinociceptive effect of spinally delivered prostaglandin E receptor antagonists in the formalin test on the rat. Neurosci Lett 173 193-196 (1994).
3  Matsuo, M., Yoshida, N., Zaitsu, M., et al. Inhibition of human glioma cell growth by a PHS-2 inhibitor, NS398, and a prostaglandin E receptor subtype EP1-selective antagonist, SC51089. Journal of Neuro-Oncology 66 285-292 (2004).
4  Carrasco, E., Casper, D., Werner, P. PGE2 receptor EP1 renders dopaminergic neurons selectively vulnerable to low-level oxidative stress and direct PGE2 neurotoxicity. J Neurosci Res 85 3109-3117 (2007).
5  Saleem, S., Li, R., Wei, G., et al. Effects of EP1 receptor on cerebral blood flow in the middle cerebral artery occlusion model of stroke in mice. J Neurosci Res 85(11) 2433-2440 (2007).


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Pricing updated 2010-03-19.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

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