ASP2905 |
Katalog-Nr.GC61960
One-Click Copy Product Info
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ASP2905 ist ein potenter und selektiver Inhibitor des Kaliumkanals Kv12.2, der durch das Kcnh3/BEC1-Gen kodiert wird.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 792184-90-8
Sample solution is provided at 25 µL, 10mM.
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ASP2905 is a novel, orally active potassium channel KCNH3 inhibitor. ASP2905 can cross the blood-brain barrier to exert antipsychotic effects, while also improving neuropsychiatric symptoms by enhancing cognitive function. ASP2905 is applicable for research in attention-deficit/hyperactivity disorder and schizophrenia[1-2].
In vitro, ASP2905 (0.1–10μM) was applied to HEK293 cells for approximately 2 days. ASP2905 bound to aptazyme- and exon skipping-based riboswitches, significantly upregulating the expression of the reporter gene EGFP, with no significant effect on the viability of HEK293 cells[3]. ASP2905 (0.1–1μM) was administered to primary cultured rat hippocampal neurons for 4 minutes. ASP2905 significantly decreased both the frequency and mean amplitude of spontaneous inhibitory postsynaptic currents (sIPSCs)[4].
In vivo, ASP2905 (0.0313–0.3 mg/kg; orally) was administered to normal ddY mice and juvenile stroke-prone spontaneously hypertensive rats (SHRSP). ASP2905 significantly shortened the finding latency in mice, prolonged the cumulative latency in rats, and concurrently increased the extracellular levels of dopamine and acetylcholine in the medial prefrontal cortex of rats, as well as the alpha band power in electroencephalograms[5]. ASP2905 (0.03–0.3mg/kg; oral administration) was used to treat a mouse model of schizophrenia. ASP2905 significantly reversed the prolonged immobility time in the forced swim test, shortened the finding latency in neonatal mice, and markedly ameliorated the hyperlocomotor activity in mice[6].
References:
[1] Nomura Y, Kim N, Zhu B, et al. Optimization of Exon-Skipping Riboswitches and Their Applications to Control Mammalian Cell Fate. ACS Synth Biol. 2024 Oct 18;13(10):3246-3255.
[2] Ishii Y, Fukunaga K, Cooney A, et al. Switchable and orthogonal gene expression control inside artificial cells by synthetic riboswitches. Chem Commun (Camb). 2024 Jun 4;60(46):5972-5975.
[3] Fukunaga K, Dhamodharan V, Miyahira N, 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.
[4] Takahashi S, Inamura K, Yarimizu J, et al. Neurochemical and neuropharmacological characterization of ASP2905, a novel potent selective inhibitor of the potassium channel KCNH3. Eur J Pharmacol. 2017 Sep 5;810:26-35.
[5] Takahashi S, Ohmiya M, Honda S, et al. The KCNH3 inhibitor ASP2905 shows potential in the treatment of attention deficit/hyperactivity disorder. PLoS One. 2018 Nov 21;13(11):e0207750.
[6] Takahashi S, Okamura A, Yamazaki M, et al. ASP2905, a specific inhibitor of the potassium channel Kv12.2 encoded by the Kcnh3 gene, is psychoactive in mice. Behav Brain Res. 2020 Jan 27;378:112315.
| Cell experiment [1]: | |
Cell lines | HEK293 cells (human embryonic kidney 293 cell line) |
Preparation Method | HEK293 cells were co-transfected with an EGFP-riboswitch plasmid containing the aptamer AC17-4 integrated into a circularly-permuted pistol (CPP) ribozyme scaffold (a8-AC17-4-CPP) in the 3' UTR, and an mCherry-expressing plasmid as a transfection control. Cells were cultured in the absence or presence of ASP2905 (0.1–10μM). |
Reaction Conditions | 0.1–10μM; 2 day. |
Applications | ASP2905 significantly activated gene expression from the riboswitch construct, leading to an approximately 10-fold upregulation of EGFP fluorescence compared to the no-ligand control. |
| Animal experiment [2]: | |
Animal models | ddY mice, juvenile stroke-prone spontaneously hypertensive rats (SHRSP) |
Preparation Method | For the water finding task, normal ddY mice were orally administered ASP2905 (0.0313 and 0.0625mg/kg) 30 minutes before a training trial. Mice were then water-deprived until the test trial on the following day. For the five-trial passive avoidance task, juvenile SHRSP rats (4 weeks old) were administered ASP2905 (0.1 and 0.3mg/kg; orally) 30 minutes before the acquisition trials. |
Dosage form | 0.0313-0.3mg/kg; p.o.; Single administration 30 minutes before behavioral testing. |
Applications | ASP2905 significantly shortened the finding latency (an index of latent learning/attention) of mice in the water finding task. ASP2905 significantly prolonged the cumulative latency of juvenile SHRSP rats (a model of ADHD) in the five-trial passive avoidance task, indicating an improvement in attention deficits and impulsivity. |
References: | |
| Cas No. | 792184-90-8 | SDF | |
| Canonical SMILES | FC1=CC=C(NC2=NC(NC3=CC=CC=C3)=NC(NCC4=NC=CC=N4)=N2)C=C1 | ||
| Formula | C20H17FN8 | M.Wt | 388.4 |
| Löslichkeit | DMSO : 100 mg/mL (257.47 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5747 mL | 12.8733 mL | 25.7467 mL |
| 5 mM | 514.9 μL | 2.5747 mL | 5.1493 mL |
| 10 mM | 257.5 μL | 1.2873 mL | 2.5747 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)