| 货号 | 14060-1mg |
| 描述 | 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 EP1receptor.1,2 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.3,4 SC-19220 also acts as a PGE2 antagonist in the EP1 receptor-mediated contraction of guinea pig trachea.5 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 EP2receptor.6,7 It binds with apparent low affinity to the cloned mouse EP1 receptor expressed in CHO cells.8 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.9 Antagonism of EP1 with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer.10 In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE2-mediated loss of dopaminergic neurons from rat substantia nigra.11 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Coleman, R.A.,Eglen, R.M.,Jones, R.L., et al. Classification of prostanoid receptors IUPHAR receptor compendium. IUPHAR Compendium 1-12 (1997). 2.Zeng, L.,An, S. and Goetzl, E.J. Selective regulation of RNK-16 cell matrix metalloproteinases by the EP4 subtype of prostaglandin E2 receptor. Biochemistry 35, 7159-7164 (1996). 3.Rakovska, A. and Milenov, K. Antagonistic effect of SC-19220 on the responses of guinea-pig gastric muscles to prostaglandins E1, E2, and F2α. Archives International Pharmacodynamics 268, 59-69 (1984). 4.Sanner, J. Prostaglandin Inhibition with a dibenzoxazepine hydrazide derivative and morphine. Annals of the New York Academy of Sciences 180, 396-409 (1971). 5.Coleman, R.A. and Kennedy, I. Characterisation of the prostanoid receptors mediating contraction of guinea-pig isolated trachea. Prostaglandins 29, 363-375 (1985). 6.Funk, C.D.,Furci, L.,Fitzgerald, G.A., et al. Cloning and expression of a cDNA for the human prostaglandin E receptor EP1 subtype. The Journal of Biological Chemisty 268, 26767-26772 (1993). 7.Bastien, L.,Sawyer, N.,Grygorczyk, R., et al. Cloning, functional expression, and characterization of the human prostaglandin E2 receptor EP2 subtype. The Journal of Biological Chemisty 269, 11873-11877 (1994). 8.Kiriyama, M.,Ushikubi, F.,Kobayashi, T., et al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. British Journal of Pharmacology 122, 217-224 (1997). 9.Inoue, H.,Tsujisawa, T.,Fukuizumi, T., et al. SC-19220, a prostaglandin E2 antagonist, inhibits osteoclast formation by 1,25-dihydroxyvitamin D3 in cell cultures. Journal of Endocrinology 161(2), 231-236 (1999). 10.Ma, X.,Kundu, N.,Ioffe, O.B., et al. Prostaglandin E receptor EP1 suppresses breast cancer metastasis and is linked to survival differences and cancer disparities. Molecular Cancer Research 8(10), 1310-1318 (2010). 11.Carrasco, E.,Casper, D. and Werner, P. PGE2 receptor EP1 renders dopaminergic neurons selectively vulnerable to low-level oxidative stress and direct PGE2 neurotoxicity. Journal of Neuroscience Research 85, 3109-3117 (2007). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥96% |
| 计算分子量 | 331.8 |
| 分子式 | C16H14ClN3O3 |
| CAS号 | 19395-87-0 |
| 稳定性 | ≥ 1 year |
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