货号 | 18115-50mg |
描述 | SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity by enhancing the degradation of HMG-CoA reductase in various animal models.1 SR-12813 is also a high affinity ligand for human and rabbit pregnane X receptors (Kd = 41 nM; EC50 = 137 nM for hPXR in vitro) and can induce cytochrome P450 3A expression in human and rabbit hepatocytes.2,3,4 |
别名 | GW 485801; |
供应商 | Cayman |
应用文献 | |
1.Berkhout, T.A.,Simon, H.M.,Patel, D.D., et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. The Journal of Biological Chemisty 271(24), 14376-14382 (1996). 2.Watkins, R.E.,Wisely, G.B.,Moore, L.B., et al. The human nuclear xenobiotic receptor PXR: Structural determinants of directed promiscuity. Science 292(5525), 2329-2333 (2001). 3.Lemaire, G.,Benod, C.,Nahoum, C., et al. Discovery of a highly active ligand of human pregnane x receptor: A case study from pharmacophore modeling and virtual screening to "in vivo" biological activity. Molecular Pharmacology 72(3), 572-581 (2007). 4.Jones, S.A.,Moore, L.B.,Shenk, J.L., et al. The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Molecular Endocrinology 14(1), 27-39 (2015). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | 22 |
纯度 | ≥98% |
计算分子量 | 504.5 |
分子式 | C24H42O7P2 |
CAS号 | 126411-39-0 |
稳定性 | ≥ 1 year |
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