SML3969

EMA401 sodium salt

≥98% (HPLC)

• Synonyme(s) : (3S)-2-(2,2-Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-iIsoquinolinecarboxylic acid, sodium salt, (3S)-EMA400 sodium salt, (3S)-PD-126,055 sodium salt, (3S)-PD-126055 sodium salt, Olodanrigan sodium salt
• Formule empirique (notation de Hill) : C₃₂H₂₈NNaO₅
• Numéro CAS: 1316755-17-5
• Poids moléculaire : 529.56
• Numéro MDL: MFCD30502664
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Conditions de stockage: desiccated
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: -10 to -25°C

Description

Actions biochimiques/physiologiques

Orally available, selective, high-affinity type-2 angiotensin II receptor (AT2R) antagonist with in vivo pain relief efficacy.



EMA401, the (3S)-enantiomer of EMA400 (PD-126,055), is a selective, high-affinity type-2 angiotensin II receptor (AT2R) antagonist (IC50 = 39.5 nM/>39 μM against 50 pM CGP 42112A for binding human AT2R/AT1R; IC50 = 39.5 nM/408 μM against 40 nM Ang II for binding rat AT2R/AT1R). EMA401, but not the AT1R antagonist losartan, is shown to inhibit capsaicin (200 nM) responses in cultured neurons of human and rat DRG (IC50  = 10 nM). EMA401 is orally available (F = 33.2%, t1/2 = 5.7 h, Cmax = 885 ng/mL post 10 mg/kg oral dosage in rats) and exhibits in vivo pain relief efficacy among adult male SD rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve (ED50 = 10 μg/kg via i.p. using the racemate EMA400).

Attention

Hygroscopic

Informations sur la sécurité

• 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