PZ0400

PF-915275

≥98% (HPLC)

• Synonyme(s) : N-(6-Amino-2-pyridinyl)-4′-cyano[1,1′-biphenyl]-4-sulfonamide; N-(6-Aminopyridin-2-yl)-4′-cyanobiphenyl-4-sulfonamide, PF 00915275, PF 915275, PF-00915275, PF00915275, PF915275
• Formule empirique (notation de Hill) : C₁₈H₁₄N₄O₂S
• CAS Number: 857290-04-1
• Poids moléculaire : 350.39
• Numéro MDL: MFCD12828758
• Code UNSPSC : 51111800
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: room temp
• Chaîne SMILES: [S](=O)(=O)(Nc3nc(ccc3)N)c1ccc(cc1)c2ccc(cc2)C#N
• InChI: 1S/C18H14N4O2S/c19-12-13-4-6-14(7-5-13)15-8-10-16(11-9-15)25(23,24)22-18-3-1-2-17(20)21-18/h1-11H,(H3,20,21,22)
• Clé InChI: ZESFDAKNYJQYKO-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1, HSD11B1) inhibitor (human 11ß-HSD1 Ki <1 nM; cellular IC₅₀ = 5 nM using human 11ß-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC₅₀ = 20/100/120 nM; mouse 11ß-HSD1 Ki = 750 nM, rat hepatoma EC50 = 14 μM). PF-915275 (0.1-3-mg/kg via nasogastric intubations) inhibits prednisone-to-prednisolone conversion in cynomolgus monkeys (by 87% with 3 mg/kg) in vivo and reduces plasma insulin increase following prednisone & resumed feeding (4 hrs post PF-915275) among overnight fasted monkeys.

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