Raloxifene 6-glucuronide
Cat. No.：YN481229
CAS No. ：174264-50-7
规格
价格(RMB)
库存
| 产品名称: | Raloxifene 6-glucuronide |
| CAS No.: | 174264-50-7 |
| Chemical Name: | 2-(4-hydroxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]benzoyl]benzo[b]thien-6-yl, β-D-glucopyranosiduronic acid |
| Synonyms: | |
| 分子量: | 649.71 |
| 分子式: | C₃₄H₃₅NO₁₀S |
| SMILES: | O[C@H]([C@H]([C@@H]([C@@H](C(O)=O)O1)O)O)[C@@H]1OC2=CC=C(C(C(C3=CC=C(OCCN4CCCCC4)C=C3)=O)=C(C5=CC=C(O)C=C5)S6)C6=C2 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Raloxifene 6-glucuronide 是 Raloxifene 的主要代谢产物。Raloxifene 6-glucuronide 的形成主要由 UGT1A1 和 UGT1A8 介导，以IC50为 290 μM 与estrogen receptor结合。 Raloxifene 是选择性非甾体雌激素受体调节剂。Raloxifene 在纳摩尔浓度激活 TGFβ3 启动子为完全激动剂，并抑制含雌激素反应元件的卵黄蛋白原启动子的表达。 |
| IC50和靶点: | |
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Sun, D., Jones, N.R., Manni, A., et al.Characterization of raloxifene glucuronidation: Potential role of UGT1A8 genotype on raloxifene metabolism in vivoCancer Prev. Res. (Phila.)6(7),719-730(2013)
Kemp, D.C., Fan, P.W., and Stevens, J.C.Characterization of raloxifene glucuronidation in vitro: Contribution of intestinal metabolism to presystemic clearanceDrug Metab. Dispos.30(6),694-700(2002)
Chae, Y.J., Kim, D.H., Lee, H.J., et al.Raloxifene inhibits cloned Kv4.3 channels in an estrogen receptor-independent mannerPflugers Arch.467(8),1663-1676(2015)
