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 |
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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].
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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].
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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. |
References |
[1]. Shinji Takahashi, 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.
[2]. Shinji Takahashi, 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. |
Molecular Formula |
C20H17FN8
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Molecular Weight |
388.40
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CAS # |
792184-90-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC1C=CC(=CC=1)NC1=NC(=NC(=N1)NCC1N=CC=CN=1)NC1C=CC=CC=1
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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.