Accéder au contenu
Merck
Toutes les photos(1)

Key Documents

View All Documentation

SML2452

Sigma-Aldrich

LY2444296

≥98% (HPLC)

Synonyme(s) :

(S)-3-Fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide, 3-Fluoro-4-[4-[[(2S)-2-(3-fluorophenyl)-1-pyrrolidinyl]methyl]phenoxy]benzamide, 4-[4-[[(2S)-2-(3-Fluorophenyl)-1-pyrrolidinyl]methyl]phenoxy]-3-fluorobenzamide, FP3FBZ, LY 2444296, LY-2444296

Se connecterpour consulter vos tarifs contractuels et ceux de votre entreprise/organisme
Toutes les photos(1)

About This Item

Formule empirique (notation de Hill):
C24H22F2N2O2
Numéro CAS:
1346133-11-6
Poids moléculaire :
408.44
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

NC(C1=CC=C(OC2=CC=C(CN3CCC[C@H]3C4=CC=CC(F)=C4)C=C2)C(F)=C1)=O

Actions biochimiques/physiologiques

LY2444296 is a brain-penetrant, orally active, short-acting, high-affinity, potent and selective κ (kappa) opioid receptor (KOR) antagonist (human κ/μ/δ Ki = 0.565/35.8/211 nM against diprenorphine binding; GTP-γ-S binding IC50/agonist/subtype transfectant = 1.57 nM/300 nM U69593/κ, 21.3 nM/1 μM DAMGO/μ 293 nM/30 nM DPDPE/d). LY2444296 reverses κ agonist antinociceptive efficacy in vivo (ED50 = 0.24 mg/kg p.o. against 1 mg/kg U69593 sc. by rat formalin test), decreases immobility time (10 or 30 mg/kg sc.) and prevents enhanced alcohol consumption (5 mg/kg i.p.) among mice subjected to stress by forced swimming.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

Charles H Mitch et al.
Journal of medicinal chemistry, 54(23), 8000-8012 (2011-10-01)
Arylphenylpyrrolidinylmethylphenoxybenzamides were found to have high affinity and selectivity for κ opioid receptors. On the basis of receptor binding assays in Chinese hamster ovary (CHO) cells expressing cloned human opioid receptors, (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide (25) had a K(i) = 0.565 nM for
Brian Reed et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 43(4), 739-750 (2017-09-01)
The κ-opioid receptor (KOP-r) system and its endogenous ligands, the dynorphins, are involved in the neurobiological regulation of addictive states, and of mood. There are limited data on the impact of selective KOP-r antagonism in humans on basic biobehavioral functions
Marta Valenza et al.
Psychopharmacology, 234(15), 2219-2231 (2017-05-28)
The recruitment of the stress circuitry contributes to a shift from positive to negative reinforcement mechanisms sustaining long-term cocaine addiction. The kappa opioid receptor (KOPr) signaling is upregulated by stress and chronic cocaine exposure. While KOPr agonists induce anhedonia and
Peng Huang et al.
European journal of pharmacology, 781, 53-59 (2016-04-06)
Kappa opioid (KOP) receptor antagonists and delta opioid (DOP) receptor agonists have antidepressant-like effects in animal tests and may be useful for treatment-resistant depression in humans. In this study, we examined whether the combination of a KOP receptor antagonist and
Peng Huang et al.
Neuroscience letters, 615, 15-20 (2016-01-19)
Prototypical long-acting kappa opioid receptor (KOPR) antagonists [e.g., norbinaltorphimine (norBNI)] have been reported to exert anxiolytic-like effects in several commonly used anxiety tests in rodents including the novelty-induced hypophagia (NIH) and elevated plus maze (EPM) tests. It remains unknown if
Afficher tous les articles scientifiques apparentés

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique