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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.
| M. Wt | 464.44 |
| Formula | C20H16F2N8.½C4H4O4 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.44 | 100 |
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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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