UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
性状
Solid
体外研究(In Vitro)
UNC10217938A strongly enhances luciferase induction in HelaLuc705 cells when used in the 5-25 μM range and are substantially more effective and potent than Retro-1. As compared to splice switching oligonucleotide (SSO) alone, UNC10217938A provids a 60-fold enhancement at 10 μM and 220-fold at 20 μM, in contrast to a 11-fold enhancement for 100 μM Retro-1.UNC10217938A can substantially enhance effects of receptor targeted oligonucleotide conjugates. UNC10217938A also can enhance effects of uncharged morpholino oligonucleotides as well as negatively charged oligonucleotides.Exposure of cells to UNC10217938A leads to a major reduction in co-localization of the TAMRA-oliogonucleotide with the late endosome marker Rab7, but had little effect on co-localization with the lysosomal marker LAMP-1. UNC10217938A causes partial release of oligonucleotide from late endosomes to t
体内研究(In Vivo)
Systemic treatment with SSO623 followed by administration of UNC10217938A (7.5 mg/kg; intravenous injection) produces distinct increases in EGFP fluorescence in liver, kidney and heart in EGFP654 mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yang B, et al. High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides. Nucleic Acids Res. 2015 Feb 27;43(4):1987-96.
溶解度数据
In Vitro: DMSO : 10 mg/mL (21.90 mM; ultrasonic and warming and heat to 80°C)配制储备液
[1]. Yang B, et al. High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides. Nucleic Acids Res. 2015 Feb 27;43(4):1987-96.