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Submit ReviewASP 7967 is a ligand for RNA aptamer AC17-4 that activates gene expression in synthetic aptazime-based riboswitches at as low as 5 μM concentration, without relying on exogenous protein factors. ASP 7967 binds aptamer AC17-4 with high affinity in HEK293 cells (Kd = 12 nM; EC50 = 2.3 μM), activating gene expression (>10-fold) in HEK293 cells. ON/OFF ratio of riboswitches activated by ASP 7967 approaches 300, with a low basal expression level in cultured cells.
In vivo, ASP 7967 upregulates the serum hEPO concentration by 7.2-fold over the vehicle control (mice). Cell permeable and low-toxic, ASP 7967 is orally bioavailable.
| 分子量 | 464.44 |
| 公式 | C20H16F2N8.½C4H4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1246958-42-8 |
| PubChem ID | 46931459 |
| InChI Key | PQVNSJGSJVAEAC-WXXKFALUSA-N |
| Smiles | FC1=CC=C(C=C1)NC2=NC(NCC3=NC=CC=N3)=NC(NC4=CC=C(F)C=C4)=N2.OC(/C=C/C(O)=O)=O.FC5=CC=C(C=C5)NC6=NC(NCC7=NC=CC=N7)=NC(NC8=CC=C(F)C=C8)=N6 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 46.44 | 100 |
以下数据基于产品分子量 464.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.77 mL | 21.53 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.31 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Salado et al (2018) Optimization of the pharmacokinetic properties of potent anti trypanosomal triazine derivatives. Eur.J.Med.Chem. 151 18 PMID: 29604541
Teixeira et al (2024) Synthetic gene circuits for regulation of next-generation cell-based therapeutics. Adv.Sci. 11 PMID: 38126677
Fukunaga et al (2023) Small-molecule aptamer for regulating RNA functions in mammalian cells and animals. J.Am.Chem.Soc. 145 7820 PMID: 36991533
Takahashi et al (2024) RNA-based controllers for engineering gene and cell therapies. Curr.Opin.Biotech. 85 PMID: 38052131
Olenginski et al (2024) Flipping the script: understanding riboswitches from an alternative perspective. J.Biol.Chem. 300 PMID: 38336293
Kläge et al (2024) A comparative survey of the influence of small self-cleaving ribozymes on gene expression in human cell culture. RNA Biology 21 1 PMID: 38146121
Wang et al (2023) Integrating ligands into nucleic acid systems. ChemBioChem 24 PMID: 37401635
If you know of a relevant reference for ASP 7967, please let us know.
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