IEM 1754 2HBr (IEM-1754; IEM 1754; IEM1754), the dihydrobromide salt of IEM-1754, is a selective voltage-dependent open-channel blocker of AMPA/kainate receptors with important biological activity. It blocks GluR1 and GluR3 with an IC50 of 6 μM.

Physicochemical Properties

Molecular Formula	C16H30N2.2HBR
Molecular Weight	412.25
Exact Mass	410.093
CAS #	162831-31-4
Related CAS #	162831-31-4
PubChem CID	9887867
Appearance	White to off-white solid powder
LogP	4.97
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	7
Heavy Atom Count	20
Complexity	233
Defined Atom Stereocenter Count	0
InChi Key	JMPHTNNJCZDROM-UHFFFAOYSA-N
InChi Code	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
Chemical Name	N'-(1-adamantylmethyl)pentane-1,5-diamine;dihydrobromide
Synonyms	IEM-1754;IEM-1754 dihydrobromide;IEM 1754; IEM1754; IEM1754 dihydrobromide; IEM-1754 2HBr;IEM 1754 dihydrobromide;IEM 1754 2HBr; IEM1754 2HBr
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In vitro activity: 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. 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
ln Vivo
Animal Protocol
References	J Physiol.1997 Dec 15;505 ( Pt 3):655-63;Br J Pharmacol.2000 Jan;129(2):265-74.

Solubility Data

Solubility (In Vitro)

DMSO: 82 mg/mL (198.9 mM) Water:82 mg/mL (198.9 mM) Ethanol:<1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.25 mg/mL (3.03 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 12.5 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: ≥ 1.25 mg/mL (3.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 1.25 mg/mL (3.03 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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W:30 mg/mL  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4257 mL	12.1286 mL	24.2571 mL
	5 mM	0.4851 mL	2.4257 mL	4.8514 mL
	10 mM	0.2426 mL	1.2129 mL	2.4257 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.