| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
ASP2905 targets the voltage-gated potassium channel Kv12.2 (KCNH3), which is encoded by the Kcnh3/BEC1 gene. KCNH3 is concentrated in the forebrain, and its overexpression in mice leads to cognitive deficits. ASP2905 is a potent inhibitor of Kv12.2, with an IC50 of 9 nM for potassium currents in CHO cells expressing Kv12.2. It is selective for Kv12.2 over other potassium channels.
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| ln Vitro |
In CHO cells expressing KCNH3, ASP2905 potently suppresses potassium currents (IC50 of 9.0 nM). 55 transmembrane proteins had modest binding affinities with ASP2905 (≤10 μM). In cultured rat hippocampus neurons, ASP2905 (0.1 µM, 1 µM) reduces the frequency of spontaneous inhibitory postsynaptic currents[1].
In vitro, ASP2905 inhibits potassium currents in CHO cells expressing Kv12.2 with an IC50 of 9 nM. The compound is a potent and selective Kv12.2 inhibitor. It shows selectivity over other potassium channel subtypes. ASP2905 can cross the blood-brain barrier (BBB), as demonstrated by its effects in CNS assays. It has antipsychotic activities and can enhance cognitive performance in preclinical models. |
| ln Vivo |
Treatment with ASP2905 prevents phencyclidine-induced hyperlocomotion. It considerably reduces the length of immobility time that phencyclidine causes in mice put through the forced swimming test[2].
In vivo, ASP2905 (orally administered) has been shown to enhance cognitive performance in animal models. It has antipsychotic activity and can cross the BBB, indicating suitability for CNS indications. Detailed in vivo efficacy data should be obtained from primary literature. The compound is typically administered orally in rodent models of psychiatric disorders or cognitive impairment. |
| Enzyme Assay |
For in vitro Kv12.2 inhibition assays, CHO cells stably expressing human or rat Kv12.2 (KCNH3) are subjected to whole-cell patch-clamp recording. Cells are held at -80 mV, and potassium currents are elicited by depolarizing voltage steps (e.g., from -80 mV to +60 mV in 10 mV increments). ASP2905 is applied at concentrations ranging from 1 pM to 100 uM. The IC50 for current inhibition is calculated by fitting dose-response curves. For selectivity, similar experiments are performed on cells expressing other potassium channel subtypes.
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| Cell Assay |
For cell-based assays, neuronal cell lines or primary neurons are treated with ASP2905 at concentrations from 1-1000 nM for 24-72 hours. Cell viability is assessed by MTT assay. For mechanistic studies, effects on neuronal firing rate, membrane potential, and action potential properties can be assessed by patch-clamp or multi-electrode array (MEA) recordings. For antipsychotic activity assessment, cells may be stimulated with dopamine or other neurotransmitters, and downstream signaling pathways (e.g., cAMP, ERK) are measured by Western blot or ELISA.
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| Animal Protocol |
Animal/Disease Models: Male ddY mice (aged 4-5 weeks) injected with Phencyclidine hydrochloride (PCP)[2]
Doses: 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg Route of Administration: Oral administration; once Experimental Results: Inhibited hyperlocomotion induced by Phencyclidine. For in vivo efficacy studies, ASP2905 is formulated in an appropriate oral vehicle (e.g., 0.5% methylcellulose or 5% DMSO in saline) and administered orally by gavage to rats or mice at doses ranging from 0.1-10 mg/kg. For cognitive enhancement studies, animals are tested in the Morris water maze, novel object recognition, or passive avoidance tasks. For antipsychotic activity, models such as amphetamine-induced hyperlocomotion, prepulse inhibition (PPI) of startle, or conditioned avoidance response (CAR) are used. Dosing is typically once daily for 1-4 weeks. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for ASP2905 are limited in publicly available sources. The compound can cross the blood-brain barrier, indicating good CNS penetration. It is described as orally active, suggesting reasonable oral bioavailability. For species-specific PK parameters (Cmax, Tmax, t1/2, oral bioavailability, brain-to-plasma ratio), researchers should consult the primary literature. Solubility: ASP2905 is soluble in DMSO up to 100 mg/mL (ultrasonic).
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| Toxicity/Toxicokinetics |
Published toxicology data for ASP2905 are limited. In animal studies at effective cognitive-enhancing or antipsychotic doses (e.g., 0.5-5 mg/kg oral), no severe adverse events have been reported. The compound is selective for Kv12.2, potentially minimizing off-target effects. Comprehensive toxicology studies have likely been conducted as part of preclinical development. Researchers should refer to primary literature for specific safety data. Standard laboratory safety precautions should be used.
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| References |
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| Additional Infomation |
ASP2905 is a research tool compound and is not approved for clinical use. It has been studied in preclinical models for its potential in cognitive enhancement and psychiatric disorders such as schizophrenia. The compound's ability to cross the BBB and its selectivity for Kv12.2 make it a valuable tool for studying the role of this potassium channel in cognitive function and psychiatric disease. ASP2905 should be stored at -20degC as a powder, protected from light and moisture.
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| Molecular Formula |
C20H17FN8
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|---|---|
| Molecular Weight |
388.40
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| Exact Mass |
388.156
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| CAS # |
792184-90-8
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| PubChem CID |
46913817
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
600.5±65.0 °C at 760 mmHg
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| Flash Point |
317.0±34.3 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.739
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| LogP |
2.26
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
463
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)NC2=NC(=NC(=N2)NCC3=NC=CC=N3)NC4=CC=C(C=C4)F
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| InChi Key |
APYUZVKHUKMAIJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17FN8/c21-14-7-9-16(10-8-14)26-20-28-18(24-13-17-22-11-4-12-23-17)27-19(29-20)25-15-5-2-1-3-6-15/h1-12H,13H2,(H3,24,25,26,27,28,29)
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| Chemical Name |
2-N-(4-fluorophenyl)-4-N-phenyl-6-N-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (257.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5747 mL | 12.8733 mL | 25.7467 mL | |
| 5 mM | 0.5149 mL | 2.5747 mL | 5.1493 mL | |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5747 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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