SC-51089

SC-51089 is an antagonist of the prostaglandin E₂ (PGE₂) receptor subtype EP₁ (K_i = 1.332 µM).¹ It is selective for EP₁ over EP₂, EP₃, and EP₄ (K_is = >100, 17.5, and >100 µM, respectively), as well as the PGD₂ receptor DP, PGF_2α receptor FP, PGI₂ receptor IP, and thromboxane A₂ receptor TP (K_is = >100, 61.13, >100, and 11.18 µM, respectively). SC-51089 (10-50 µM) decreases cell death induced by amyloid-β 1-42 (Aβ42) in MC65 human neuroblastoma cells.² It inhibits the growth of KMG-4 glioma cells in vitro (IC₅₀ = ~1 µM) and reduces tumor growth in a KMG4 mouse xenograft model when administered at a dose of 25 mg/kg.³ SC-51089 also reduces phenylbenzoquinone-induced writhing in mice (ED₅₀ = 6.8 mg/kg).⁴

WARNING This product is not for human or veterinary use.

1. Abramovitz, M., Adam, M., Boie, Y., et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim. Biophys. Acta 1483(2), 285-293 (2000).

2. Li, X., Rose, S.E., Montine, K.S., et al. Antagonism of neuronal prostaglandin E₂ receptor subtype 1 mitigates amyloid β neurotoxicity in vitro. J. Neuroimmune Pharmacol. 8(1), 87-93 (2016).

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. J. Neurooncol. 66, 285-292 (2004).

4. 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).

An, Y., Belevych, N., Wang, Y., et al. Neuronal and nonneuronal COX-2 expression confers neurotoxic and neuroprotective phenotypes in response to excitotoxin challenge. J. Neurosci. Res. 92(4), 486-495 (2014).