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Merck
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SML2417

Sigma-Aldrich

ORG 25543 Hydrochloride

≥95% (HPLC)

Sinonimo/i:

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

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About This Item

Formula empirica (notazione di Hill):
C24H32N2O4·HCl
Numero CAS:
495076-64-7
Peso molecolare:
448.98
Numero MDL:
MFCD23701926
Codice UNSPSC:
12352200
NACRES:
NA.77

Saggio

≥95% (HPLC)

Forma fisica

powder

Condizioni di stoccaggio

desiccated

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

room temp

InChI

1S/C24H32N2O4.ClH/c1-26(2)24(12-8-9-13-24)17-25-23(27)19-14-20(28-3)22(21(15-19)29-4)30-16-18-10-6-5-7-11-18;/h5-7,10-11,14-15H,8-9,12-13,16-17H2,1-4H3,(H,25,27);1H
NIPQJILJYQVZJR-UHFFFAOYSA-N

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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Katsuya Morita et al.
The Journal of pharmacology and experimental therapeutics, 326(2), 633-645 (2008-05-02)
Neuropathic pain is refractory against conventional analgesics, and thus novel medicaments are desired for the treatment. Glycinergic neurons are localized in specific brain regions, including the spinal cord, where they play an important role in the regulation of pain signal
A Mingorance-Le Meur et al.
British journal of pharmacology, 170(5), 1053-1063 (2013-08-22)
Available medications for chronic pain provide only partial relief and often cause unacceptable side effects. There is therefore a need for novel molecular targets to develop new therapeutics with improved efficacy and tolerability. Despite encouraging efficacy data in rodents with
Cristina Romei et al.
Neurochemistry international, 99, 169-177 (2016-07-11)
Glycine can be substrate for two transporters: GlyT1, largely expressed by astrocytes but also by some non-glycinergic neurons, and GlyT2, most frequently present in glycine-storing nerve endings. In morphological studies, GlyT2 expression had been found to be restricted to caudal
M A Gradwell et al.
The Journal of physiology, 595(23), 7185-7202 (2017-09-15)
Spinal parvalbumin-expressing interneurons have been identified as a critical source of inhibition to regulate sensory thresholds by gating mechanical inputs in the dorsal horn. This study assessed the inhibitory regulation of the parvalbumin-expressing interneurons, showing that synaptic and tonic glycinergic
France Rousseau et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 28(39), 9755-9768 (2008-09-26)
At inhibitory synapses, glycine and GABA are accumulated into synaptic vesicles by the same vesicular transporter VGAT/VIAAT (vesicular GABA transporter/vesicular inhibitory amino acid transporter), enabling a continuum of glycine, GABA, and mixed phenotypes. Many fundamental aspects of the presynaptic contribution
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