(20E)-17α,20-[(1-メトキシエタン-1,1-ジイル)ビスオキシ]-3-オキソ-19-ノルプレグナ-4,20-ジエン-21-カルボン酸メチル 化学特性,用途語,生産方法
説明
YK11 was first studied by Japanese researcher Yuichiro Kanno in 2011. It was found to be a partial agonist of the androgen receptor (AR), genetically selective, leading researchers to believe the compound was a SARM. YK11 is an experimental drug candidate and an unapproved substance for use in humans.
使用
YK-11 is a synthetic steroidal selective androgen receptor modulator (SARM).It is a gene-selective partial agonist of the androgen receptor (AR) and does not induce the physical interaction between the NTD/AF1 and LBD/AF2 (known as the N/C interaction), which is required for full transactivation of the AR.
作用機序
YK-11 is an androgen receptor partial agonist that activates androgen receptor transcriptional activity in HEK293 cells overexpressing androgen receptors when used at a concentration of 0.1 μM.1 It induces expression of the androgen receptor target genes FKBP51 and FGF18 in HEK293 cells when used at a concentration of 10 μM. YK-11 accelerates nuclear translocation of androgen receptors without inducing interaction between the androgen receptor N- and C-termini. In C2C12 cells, YK-11 (500 nM) increases expression of the myogenic regulatory factors MyoD, Myf5, and myogenin, as well as follistatin (Fst), and induces myogenic differentiation.
参考文献
[1] Yuichiro Kanno, et al. Exp Cell Res. Differential DNA-binding and cofactor recruitment are possible determinants of the synthetic steroid YK11-dependent gene expression by androgen receptor in breast cancer MDA-MB 453 cells DOI:
10.1016/j.yexcr.2022.113333[2] Su Jin Lee, et al. Biochem Biophys Res Commun. Myostatin inhibitor YK11 as a preventative health supplement for bacterial sepsis DOI:
10.1016/j.bbrc.2021.01.030[3] Tomofumi Yatsu, et al. Biol Pharm Bull. Selective Androgen Receptor Modulator, YK11, Up-Regulates Osteoblastic Proliferation and Differentiation in MC3T3-E1 Cells DOI:
10.1248/bpb.b17-00748[4] Mario Thevis, et al. Mol Cell Endocrinol. Detection of SARMs in doping control analysis DOI:
10.1016/j.mce.2017.01.040[5] Yuichiro Kanno, et al. Biol Pharm Bull. Selective androgen receptor modulator, YK11, regulates myogenic differentiation of C2C12 myoblasts by follistatin expression DOI:
10.1248/BPB.B13-00231
(20E)-17α,20-[(1-メトキシエタン-1,1-ジイル)ビスオキシ]-3-オキソ-19-ノルプレグナ-4,20-ジエン-21-カルボン酸メチル 上流と下流の製品情報
原材料
準備製品