IEM 1754 2HBr

Catalog No.S2860

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

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IEM 1754 2HBr Chemical Structure

IEM 1754 2HBr Chemical Structure
Molecular Weight: 412.25

Validation & Quality Control

Quality Control & MSDS

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Product Description

Biological Activity

Description IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
Targets GluR1 [1] GluR3 [1]
IC50 6 μM 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]
In vivo

Protocol(Only for Reference)

Kinase Assay: [1]

Electrophysiological recording from oocytes 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Magazanik LG, et al. J Physiol, 1997, 505( Pt 3), 655-663.

[2] Tikhonov DB, et al. Br J Pharmacol, 2000, 129(2), 265-274.

Chemical Information

Download IEM 1754 2HBr SDF
Molecular Weight (MW) 412.25


CAS No. 162831-31-4
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 82 mg/mL (198.9 mM)
Water 82 mg/mL (198.9 mM)
Ethanol <1 mg/mL
* <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.
Chemical Name 1,5-Pentanediamine, N1-(tricyclo[,7]dec-1-ylmethyl)-, hydrobromide (1:2)

Tech Support

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