ASP 7967

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Description: Ligand for RNA aptamer AC17-4 activating gene expression in aptazime-based riboswitches
Chemical Name: N2,N4-Bis(4-fluorophenyl)-N6-(2-pyrimidinylmethyl)-1,3,5-triazine-2,4,6-triamine hemifumarate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for ASP 7967

ASP 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.

Technical Data for ASP 7967

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.

Solubility Data for ASP 7967

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.44 100

Preparing Stock Solutions for ASP 7967

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for ASP 7967

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


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Citations for ASP 7967

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Literature in this Area

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