PZ0206

PF-04455242 hydrochloride

≥98% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₁H₂₈N₂O₂S · HCl
• CAS Number: 1322001-35-3
• Molecular Weight: 408.99
• MDL number: MFCD22666388
• UNSPSC Code: 51111800
• PubChem Substance ID: 329823774
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: 5 mg/mL (clear solution, warmed)
• storage temp.: 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
• InChI key: WRNZYMZEVIVCFL-UHFFFAOYSA-N

Description

Biochem/physiol Actions

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.

Features and Benefits

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable