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IEM 1754 dihydrobroMide

CAS# 162831-31-4

IEM 1754 dihydrobroMide

Catalog No. BCC5049----Order now to get a substantial discount!

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IEM 1754 dihydrobroMide: 5mg $46 In Stock
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Chemical structure

IEM 1754 dihydrobroMide

3D structure

Chemical Properties of IEM 1754 dihydrobroMide

Cas No. 162831-31-4 SDF Download SDF
PubChem ID 9887867 Appearance Powder
Formula C16H32Br2N2 M.Wt 412.25
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 50 mM in DMSO
Chemical Name N'-(1-adamantylmethyl)pentane-1,5-diamine;dihydrobromide
SMILES C1C2CC3CC1CC(C2)(C3)CNCCCCCN.Br.Br
Standard InChIKey JMPHTNNJCZDROM-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H30N2.2BrH/c17-4-2-1-3-5-18-12-16-9-13-6-14(10-16)8-15(7-13)11-16;;/h13-15,18H,1-12,17H2;2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of IEM 1754 dihydrobroMide

DescriptionVoltage-dependent open-channel blocker of AMPA receptors. Selective between subtypes; blocks GluR2 subunit-lacking (Ca2+-permeable) receptors more potently than GluR2-containing receptors. Also potently blocks NMDA receptor channels. Less sensitive than IEM at a holding potential between -40 and -80mV.

IEM 1754 dihydrobroMide Dilution Calculator

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IEM 1754 dihydrobroMide Molarity Calculator

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Preparing Stock Solutions of IEM 1754 dihydrobroMide

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4257 mL 12.1286 mL 24.2571 mL 48.5143 mL 60.6428 mL
5 mM 0.4851 mL 2.4257 mL 4.8514 mL 9.7029 mL 12.1286 mL
10 mM 0.2426 mL 1.2129 mL 2.4257 mL 4.8514 mL 6.0643 mL
50 mM 0.0485 mL 0.2426 mL 0.4851 mL 0.9703 mL 1.2129 mL
100 mM 0.0243 mL 0.1213 mL 0.2426 mL 0.4851 mL 0.6064 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on IEM 1754 dihydrobroMide

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

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References on IEM 1754 dihydrobroMide

Voltage-dependent block of native AMPA receptor channels by dicationic compounds.[Pubmed:10694232]

Br J Pharmacol. 2000 Jan;129(2):265-74.

1. The kinetics of open channel block of GluR2-containing and GluR2-lacking AMPA receptors (AMPAR) by dicationic compounds (IEM-1460, IEM-1754, and IEM-1925) have been studied in rat hippocampal neurones using whole-cell patch clamp recording and concentration-jump techniques. Neurones were isolated from hippocampal slices by vibrodissociation. 2. The dicationic compounds were approximately 100 - 200 times more potent as blockers of GluR2-lacking AMPAR than as blockers of GluR2-containing AMPAR. The subunit specificity of channel block is determined by the blocking rate constant of a dicationic compound, whereas differences in unblocking rate constants account for differences in potency. 3. Hyperpolarization may decrease the block produced by IEM-1460 and IEM-1754 block due to the voltage-dependence of the unblocking rate constants for these compounds. This suggests that dicationic compounds permeate the AMPAR channel at negative membrane potentials. The effect was particularly apparent for GluR2-lacking AMPAR. These findings indicate that the presence of GluR2-subunit(s) in AMPAR hinders the binding of the cationic compounds and their permeation through the channel. 4. The most potent compound tested was IEM-1925. The presence of a phenylcyclohexyl moiety instead of an adamantane moiety, as in IEM-1460 and IEM1754, is probably responsible for the higher potency of IEM-1925. Dicationic compounds are important not only as pharmacological tools, but also as templates for the synthesis of new selective AMPAR blockers which may be potential therapeutic agents.

Block of open channels of recombinant AMPA receptors and native AMPA/kainate receptors by adamantane derivatives.[Pubmed:9457643]

J Physiol. 1997 Dec 15;505 ( Pt 3):655-63.

1. The effects of two adamantane derivatives, 1-trimethylammonio-5-(1-adamantane-methyl-ammoniopentane dibromide) (IEM-1460) and 1-ammonio-5-(1-adamantane-methylammoniopentane dibromide) (IEM-1754) on kainate-induced currents were studied in Xenopus oocytes expressing recombinant ionotropic glutamate receptors and in freshly isolated neurones from rat hippocampal slices. 2. The adamantane derivatives caused use- and voltage-dependent block of open channels of recombinant AMPA receptors. This antagonism was dependent on receptor subunit composition; channels gated by recombinant, homomeric GluR1 and GluR3 receptors exhibited a higher sensitivity to block than those gated by receptors containing edited GluR2 subunits. In the former cases, IEM-1460 had an IC50 of 1.6 microM at a holding potential (Vh) of -80 mV and IEM-1754 was 3.8 times less potent than IEM-1460. In contrast, 100 microM IEM-1460 inhibited responses to 100 microM kainate of receptors containing edited GluR2 subunits by only 7.8 +/- 2.4% (n = 5 oocytes at a Vh of -80 mV. 3. Native AMPA/kainate receptors in isolated hippocampal cells were inhibited by adamantane derivatives in a use- and voltage-dependent manner. This antagonism was dependent on cell type: pyramidal neurones were less sensitive to IEM-1460 (IC50 = 1617 microM at Vh = -80 mV) than interneurones (IC50 = 1.6 microM at Vh = -80 mV). IEM-1460 and IEM-1754 were equipotent when applied to pyramidal neurones, but IEM-1754 was less potent (approximately 3 times) than IEM-1460 when applied to interneurones. 4. It is concluded that the presence of the edited GluR2 subunit in recombinant AMPA receptors and native AMPA/kainate receptors inhibits channel block by organic cations and that adamantane derivatives are potentially valuable tools for identifying classes of AMPA/kainate receptors and their roles in synaptic transmission.

Description

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

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