product name IEM 1754 2HBr
Description: IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM. IEM 1754 causes use- and voltage-dependent block of open channels of recombinant AMPA receptors. 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.
References: J Physiol. 1997 Dec 15;505 ( Pt 3):655-63; Br J Pharmacol. 2000 Jan;129(2):265-74.
412.25
Formula
C16H30N2.2HBr
CAS No.
162831-31-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 82 mg/mL (198.9 mM)
Water: 82 mg/mL (198.9 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423517
| In 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 Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Physiol. 1997 Dec 15;505 ( Pt 3):655-63; Br J Pharmacol. 2000 Jan;129(2):265-74. |
Plerixafor (octahydrochloride)
