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G5918

Sigma-Aldrich

GR 113808

≥98% (HPLC), solid

Sinonimo/i:

1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate

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About This Item

Formula empirica (notazione di Hill):
C19H27N3O4S
Numero CAS:
144625-51-4
Peso molecolare:
393.50
Numero MDL:
MFCD00912901
Codice UNSPSC:
12352200
ID PubChem:
24278311
NACRES:
NA.77

Saggio

≥98% (HPLC)

Stato

solid

Colore

white to light pink

Solubilità

DMSO: >20 mg/mL

Ideatore

GlaxoSmithKline

Temperatura di conservazione

2-8°C

Stringa SMILE

Cn1cc(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)c3ccccc13

InChI

1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3
MOZPSIXKYJUTKI-UHFFFAOYSA-N

Informazioni sul gene

human ... HTR4(3360)
rat ... Htr3a(79246) , Htr4(25324)

Applicazioni

GR 113808 has been used as a serotonin receptor 4 (5-HT4R) blocker to study its effects on the calcium (Ca2+) transients in rat ventricular cardiomyocytes. It has also been used as a 5-HT4R antagonist to study its effects on de novo enteric neurogenesis in post-embryonic zebrafish.

Azioni biochim/fisiol

GR 113808 is a 5-HT4 serotonin receptor antagonist.

Caratteristiche e vantaggi

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Note legali

Sold for research purposes under agreement from Glaxo­Smith­Kline

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

Dispositivi di protezione individuale

Eyeshields, Gloves, type N95 (US)

Scegli una delle versioni più recenti:

Certificati d'analisi (COA)

Lot/Batch Number
BGBC4521
128K4613V
128K46132
128K46131
128K4613

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Sigma-Aldrich

Sigma-Aldrich

H6648

Hanks′ Balanced Salt solution

Poli(etilenglicole) 400, for synthesis

Sigma-Aldrich

8.07485

Poli(etilenglicole)

Dispase® II (neutral protease, grade II) lyophilized, from bacterial, Roche, pkg of 5 × 1 g

Roche

04942078001

Dispase® II (neutral protease, grade II)

A N James et al.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society, 17(1), 76-82 (2005-01-27)
Selective serotonin reuptake inhibitors (SSRIs) are increasingly used to treat a variety of disorders but have gastrointestinal side-effects. To determine the effects of the SSRI, fluoxetine, on gastric smooth muscle contractility. Fundic, antral, and pyloric circular muscle contractility of guinea
Lucie Rivail et al.
British journal of pharmacology, 143(3), 361-370 (2004-09-08)
A body of evidences suggests that a hydrophobic pocket of the human 5-HT(4) receptor contributes to the high affinity of some bulky 5-HT(4) ligands. A thorough study of this pocket was performed using mutagenesis and molecular modeling. Ligand binding or
Guillaume Lucas et al.
Biological psychiatry, 57(8), 918-925 (2005-04-12)
We recently identified a facilitory control exerted by serotonin4 (5-HT4) receptors on the in vivo firing activity of dorsal raphe nucleus (DRN) serotonergic (5-HT) neurons. However, these findings were based on acute administrations of 5-HT4 receptor agonists and antagonists, which
J Kamei et al.
Neuroscience, 174, 224-233 (2010-11-18)
Respiratory depression is the most well-known and dangerous side-effect of opioid analgesics. Clinical investigations have revealed that this opioid-induced respiratory depression is less severe in patients with chronic pain, but the mechanisms that underlie this phenomenon are unknown. Therefore, the
Tadayoshi Mikami et al.
Journal of pharmacological sciences, 107(3), 251-259 (2008-07-01)
In the present study, binding affinities of 5-hydroxytryptamine-4 (5-HT(4)) ligands for the human 5-HT(4d) receptor were determined using the agonist [(3)H]5-HT and the selective 5-HT(4) antagonist [(3)H]GR113,808. We also compared the affinity differences between [(3)H]5-HT binding (K(H)) and [(3)H]GR113,808 binding
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