IEM 1754 2HBr

製品コードS2860 バッチS286002

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₆H₃₀N₂.2HBr
	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.

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生物活性

製品説明	IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
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]

製品説明

IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

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]

プロトコル(参考用のみ)

キナーゼアッセイ	Electrophysiological recording from oocytes
キナーゼアッセイ	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.

参考

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。

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