Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

被引：54

作者：

Miller, Chris P. ^{[1
]}

Shomali, Maysoun ^{[1
]}

Lyttle, C. Richard ^{[1
]}

O'Dea, Louis St. L. ^{[1
]}

Herendeen, Hillary ^{[1
]}

Gallacher, Kyla ^{[1
]}

Paquin, Dottie ^{[1
]}

Compton, Dennis R. ^{[2
]}

Sahoo, Bishwabhusan ^{[2
]}

Kerrigan, Sean A. ^{[2
]}

Burge, Matthew S. ^{[2
]}

Nickels, Mictiael ^{[2
]}

Green, Jennifer L. ^{[2
]}

Katzenellenbogen, John A. ^{[3
]}

Tchesnokov, Alexei ^{[4
]}

Hattersley, Gary ^{[1
]}

机构：

[1] Radius Hlth Inc, Cambridge, MA 02139 USA

[2] Obiter Res, Champaign, IL 61822 USA

[3] Univ Illinois, Dept Chem, Urbana, IL 61801 USA

[4] Cambridge Major Labs Inc, Germantown, WI 53022 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2011年 / 2卷 / 02期

关键词：

Androgen; SARM; cachexia; oxadiazole; Herschberger assay; primate; MUSCLE; POTENT;

D O I：

10.1021/ml1002508

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.

引用

页码：124 / 129

页数：6

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