Synonym: 4-Benzyloxy-3,5-dimethoxy-N-[(1-dimethylaminocyclopentyl)methyl]benzamide hydrochloride; N-[[1-(Dimethylamino)cyclopentyl]methyl]-3,5-dimethoxy-4-(phenylmethoxy)benzamide hydrochloride; ORG 25,543 hydrochloride; ORG 25543 hydrochloride; ORG-25543 hydrochloride
CAS Number: 495076-64-7
Empirical Formula (Hill Notation): C24H32N2O4·HCl
Molecular Weight: 448.98
MDL Number: MFCD23701926
Linear Formula: C24H32N2O4·HCl
Product Type: Chemical
assay |
≥95% (HPLC) |
color |
white to beige |
form |
powder |
solubility |
DMSO: 2 mg/mL, clear |
storage condition |
desiccated |
storage temp. |
room temp |
Biochem/physiol Actions: |
ORG 25543 is a brain-penetrant (free brain/plasma ratio = 0.53; 35 min post 2 or 20 mg/kg i.v. in mice), high-affinity, potent and selective glycine transporter 2 (GlyT-2; GlyT2) inhibitor (human & mouse pIC50 = 7.9/ GlyT2 vs <4/GlyT1) with great selectivity over a panel of 56 receptor and channel proteins. ORG 25543 is more potent and selective than the brain-impermeable ALX-1393 (GlyT2/GlyT1 pIC50 = 7.1/5.4) and exhibits high in vivo efficacy in a murine diabetic neuropathic pain model (ED50 = 0.07-0.16 mg/kg i.v.; Emin = 0.01 mg/kg). ORG 25543 is practically irreversible due to its tight-binding nature, suboptimal dosage should be applied in vivo to allow low target occupancy only and minimize acute toxicity. |
WGK Germany |
WGK 3 |
Flash Point(F) |
Not applicable |
Flash Point(C) |
Not applicable |
Purity |
≥95% (HPLC) |
Storage Temp. |
room temp |
UNSPSC |
12352200 |