申请人:Miltenyi Biotec GmbH
公开号:EP2781523A1
公开(公告)日:2014-09-24
Lipophilic oligonucleotide comprising a phosphate glycerol unit containing at least one aliphatic unsaturated carbon bond according to formula I
with
Oligonucleotide =
an unmodified or modified nucleic acid of 2 - 1000 nucleotides in length
R =
a bond or a linker unit
Y =
OH, SH or NHR3
X and Z =
independently O, S or NR3
R3 =
hydrogen or branched or unbranched and/or substituted or unsubstituted alkyl, aryl and/or alkyl aryl residue with 10 to 30 carbon atoms
R1, R2 =
branched or unbranched and/or substituted or unsubstituted alkyl, aryl and/or alkylaryl residue with 10 to 30 carbon atoms, with the provisio that at least one of the residues R1 or R2 comprises at least one aliphatic carbon-carbon double bond
Use of lipophilic oligonucleotide according to Formula I for drug discovery or for transfection of cells.
亲脂性寡核苷酸,包含一个磷酸甘油单元,该单元含有至少一个脂肪族不饱和碳键,如式 I 所示
式中
寡核苷酸 =
长度为 2 - 1000 个核苷酸的未修饰或修饰的核酸
R =
键或连接单元
Y =
OH、SH 或 NHR3
X 和 Z =
独立的 O、S 或 NR3
R3 =
氢或支链或未支链和/或具有 10 至 30 个碳原子的取代或未取代的烷基、芳基和/或烷基芳基残基
R1、R2 =
具有 10 至 30 个碳原子的支链或未支链和/或取代或未取代的烷基、芳基和/或 烷芳基残基,但 R1 或 R2 残基中至少有一个包含至少一个脂肪族碳-碳双键
将符合式 I 的亲脂寡核苷酸用于药物开发或细胞转染。