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SML2417 Sigma-Aldrich

ORG 25543 Hydrochloride

≥95% (HPLC)

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

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, O
assay   ≥95% (HPLC)
form   powder
storage condition   desiccated
color   white to beige
solubility   DMSO: 2 mg/mL, clear
storage temp.   room temp

Description

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.

Safety & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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