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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H30N2.2HBr |
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分子量 | 412.25 | CAS No. | 162831-31-4 | |
Solubility (25°C)* | 体外 | DMSO | 82 mg/mL (198.9 mM) | |
Water | 82 mg/mL (198.9 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM. |
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in vitro | IEM 1754 is an adamantane derivative. IEM 1754 causes use- and voltage-dependent block of open channels of recombinant AMPA receptors. This antagonism is dependent on receptor subunit composition, channels gated by recombinant, homomeric GluR1 and GluR3 receptors exhibites a higher sensitivity to block than those gated by receptors containing edited GluR2 subunits. [1] IEM-1754 block of GluR2-containing AMPAR is enhanced by hyperpolarization in agreement with the classical single-exponential model. In contrast, the block of GluR2-lacking AMPAR is reduced by hyperpolarization. [2] |
キナーゼアッセイ | Electrophysiological recording from oocytes | |
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Four to seven days after injection of GluR1, GluR2 and GluR3 mRNA, oocytes are placed in a Silicone tube of 2 mm diameter and continuously perfused with saline (120 mM NaCl, 2 mM KCI, 1.8 mM CaCl2 and 9.5 mM Hepes, pH 7.4) at 22-24 °C. Currents elicited by 100 μM kainite are measured using a conventional two-microelectrode voltage clamp. Each application of kainate lasts 20-40 s. When the current induced by this agonist reaches a steady state, the saline flow is switched to a solution containing the same concentration of kainate plus a given concentration of IEM-1754. Again, on reaching a steady state, the saline flow is returned to a solution containing kainate alone when recovery of the response to the agonist is recorded. This procedure is repeated several times, at not less than 5 min intervals, with different concentrations of the adamantane derivative. It is possible to conduct several experiments on a single oocyte. Unless otherwise noted, membrane currents are measured at a holding potential (Vh) of -80 mV. The voltage dependence of antagonism is estimated by ramping the membrane potential from -140 mV to +40 mV, the duration of the ramp being 20 s. Voltage and current responses are recorded on magnetic tape and post-analysed using in-house software. |
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長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。