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SC-51089

Cayman Chemical Item Number 10011561

CID132748 (CAS 146033-02-5)

SC-51089 (CAS 146033-02-5)

See more	Inhibitors (493) Cancer (606) Pain (144)

Description

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

4 Carrasco, E., Casper, D., and 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).

Synonyms	CID132748
Formal Name	8-chloro-2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, monohydrochloride
CAS Number	146033-02-5
Molecular Formula	C₂₂H₁₉ClN₄O₃ · HCl
Formula Weight	459.3
Formulation	A crystalline solid
Purity	≥95%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard O=C(CCc1ccncc1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc12

Background Reading

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).

Malmberg, A.B., Rafferty, M.F., and 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).

Carrasco, E., Casper, D., and 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).

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).

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).

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Size	Price	Quantity	Subtotal
1 mg	$15.00		$0.00
5 mg	$68.00		$0.00
10 mg	$129.00		$0.00
25 mg	$263.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-09. Prices are subject to change without notice.

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