(R)-Butaprost free acid (货号:AYB28082)
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生物活性
产品信息
生物活性
| 生物活性 | (R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.) |
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| CAS | 215168-33-5 |
| 中文名称 | (R)-普鲁前列素,游离酸 |
| 分子量 | 394.54 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 保存条件 | Please store the product under the recommended conditions in the Certificate of Analysis. |
产品信息
| Intro | (R)-Butaprost (free acid)。Butaprost 是前列腺素 E2 (PGE2) 的结构类似物，对 EP2 受体亚型具有良好的选择性。布他前列素经常用于药理学定义各种人类和动物组织和细胞的 EP 受体表达谱。 Gardiner 在 1986 年引起了对布他前列素结构的严重混淆，当时他报告说显示这种选择性活性的布他前列素差向异构体是 C-16 (R)-差向异构体（参见参考文献 2 和注释）。为了增加 (R)-butaprost 对前列腺素受体的结合亲和力，我们去除了 (R)-butaprost 的甲酯并重新建立了天然的 C-1 羧酸。前列腺素游离酸通常以相应酯衍生物的 10 到 100 倍的亲和力与其同源受体结合。 (R)-butaprost 的药理学尚未经过仔细研究，但通常认为它是活性较低的 C-16 差向异构体。 （注意：在 1986 年英国药理学杂志的 Gardiner 论文中，布他前列素出现在第 46 页，其名称为 TR 4979。所绘制的结构不正确，因为作者使用并指的是活性更强的 C- 16 差向异构体，实际上是 16(S)。46 页的结构显示结构为 16(R)。直到 1990 年代后期，美国和日本的仔细研究才正确地确定了 C-16 的实际构型在称为布他前列素的化合物中是 16(S)。） |
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| 别名 | (R)-普鲁前列素,游离酸 |