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Art. -Nr.: HY-49538C

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ASP7967 hemifumarate

ASP7967 hemifumarate is an orally active ligand of the RNA aptamer AC17-4 with a K_d of 12 nM. ASP7967 hemifumarate binds AC17-4 to regulate aptazyme-based and exon-skipping riboswitches, thereby enabling small-molecule-controlled transgene expression without exogenous protein factors. ASP7967 hemifumarate can be used for the study of synthetic RNA switches, gene expression regulation and AAV-based gene therapy-related expression control.

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CAS. Nr.: 1246958-42-8
Formel: C₂₄H₂₀F₂N₈O₄
Molecular Weight:464.43

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ASP7967 hemifumarate Chemical Structure

CAS. Nr.: 1246958-42-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

AC17-4 aptamer

12 nM (Kd)

In Vitro

ASP7967 hemifumarate binds the RNA aptamer AC17-4 with a K_d of 12 nM^[1].
ASP7967 (5 μM; 2 days after transfection) hemifumarate activates EGFP expression by approximately 10-fold in HEK293 cells expressing the a8-AC17-4-CPP aptazyme riboswitch^[1].
ASP7967 (10 μM; 2 days after transfection) hemifumarate mostly saturates the a8-AC17-4-CPP riboswitch response in HEK293 cells, with an EC₅₀ of approximately 2.3 μM and a fully induced ON level of approximately 50% of the empty-vector control^[1].
ASP7967 (0-10 μM; 18 h) hemifumarate does not significantly reduce HEK293 cell viability in the MTT assay^[1].
ASP7967 (0.1-10 μM; 2 days after transfection) hemifumarate regulates hEPO secretion from HEK293 cells transfected with pAAV-CMV-hEPO-a8c-AC17-4-CPP, at 10 μM, it upregulates hEPO secretion by approximately 10-fold, reaching 29% of the no-riboswitch control construct^[1].
ASP7967 hemifumarate triggers EGFP expression via riboswitches with ON/OFF ratios of 114, 58 and 177 respectively in HEK293 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ELISA Assay^[1]

Cell Line:

HEK293
Concentration:

10 μM
Incubation Time:

2 days after transfection
Result:

Upregulated hEPO secretion by approximately 10-fold in cells transfected with pAAV-CMV-hEPO-a8c-AC17-4-CPP.
Increased hEPO secretion to 29% of the no-riboswitch control construct.

Cell Viability Assay^[1]

Cell Line:

HEK293
Concentration:

0, 2, 5, 10 µM
Incubation Time:

2 days after transfection
Result:

Did not significantly reduce HEK293 cell viability in the MTT assay.

Parmacokinetics

Species	Dose	Route	T_max
Mice^[1]	100 mg/kg	p.o.	1 h

In Vivo

ASP7967 (100 mg/kg; p.o.; single administration, 2 weeks after AAV injection; blood collected at 2,4,6,8,24 h postdose) hemifumarate upregulates serum hEPO in BALB/c mice injected with 3 × 10¹⁰ GC AAV8-CMV-hEPO-a8c-AC17-4-CPP; serum hEPO peaks at ~115 mIU/mL (6-8 h) with a 7.2-fold elevation vs vehicle, while no hEPO change occurs in mice receiving control AAV8-CMV-hEPO^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

7-week-old male BALB/c mice intravenously injected with 3 × 10¹⁰ genome copies of AAV8-CMV-hEPO-a8c-AC17-4-CPP per mouse^[1]
Dosage:

100 mg/kg
Administration:

Oral administration (p.o.); single administration; 2 weeks after AAV injection
Result:

Upregulated serum hEPO expression in mice.
Increased serum hEPO to approximately 115 mIU/mL at 6-8 h postdosing.
Produced a 7.2-fold increase in serum hEPO over vehicle control.
Serum hEPO subsequently decreased in accordance with the decline of ASP7967 concentration in the liver.

Chemical Information

CAS. Nr. 1246958-42-8
Molecular Weight 464.43
Formel C₂₄H₂₀F₂N₈O₄
SMILES

OC(/C=C/C(O)=O)=O.FC(C=C1)=CC=C1NC2=NC(NC3=CC=C(C=C3)F)=NC(NCC4=NC=CC=N4)=N2.[1/2]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Fukunaga K et al. Small-Molecule Aptamer for Regulating RNA Functions in Mammalian Cells and Animals. J Am Chem Soc. 2023 Apr 12;145(14):7820-7828. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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