PZ0206

PF-04455242 hydrochloride

≥98% (HPLC)

• Synonym(e): 2-Methyl-N-((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine hydrochloride, N-(2-Methylpropyl)-2′-(1-pyrrolidinylsulfonyl)-[1,1′-biphenyl]-4-methanamine hydrochloride, PF-4455242 hydrochloride
• Empirische Formel (Hill-System): C₂₁H₂₈N₂O₂S · HCl
• CAS-Nummer: 1322001-35-3
• Molekulargewicht: 408.99
• MDL-Nummer: MFCD22666388
• UNSPSC-Code: 51111800
• PubChem Substanz-ID: 329823774
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Lagerbedingungen: desiccated
• Farbe: white to beige
• Löslichkeit: DMSO: 5 mg/mL (clear solution, warmed)
• Lagertemp.: room temp
• SMILES String: Cl.CC(C)CNCc1ccc(cc1)-c2ccccc2S(=O)(=O)N3CCCC3
• InChI: 1S/C21H28N2O2S.ClH/c1-17(2)15-22-16-18-9-11-19(12-10-18)20-7-3-4-8-21(20)26(24,25)23-13-5-6-14-23;/h3-4,7-12,17,22H,5-6,13-16H2,1-2H3;1H
• InChIKey: WRNZYMZEVIVCFL-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

PF-4455242 is a selective k opioid receptor (KOR) antagonist with 20-fold selectivity for kappa over mu receptors (k Ki = 3 nM, μ Ki =64 nM). PF-4455242 is orally active, has good brain penetration in rats and was able to block the effects of the kappa agonist U50488. Studies indicate that k blockade has afforded antidepressant activity in several animal models. PF-4455242 has been in phase I clinical trials for trial for bipolar depression.

Leistungsmerkmale und Vorteile

This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable