PZ0206

PF-04455242 hydrochloride

≥98% (HPLC)

• 別名: 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
• 実験式（ヒル表記法）: C₂₁H₂₈N₂O₂S · HCl
• CAS番号: 1322001-35-3
• 分子量: 408.99
• MDL番号: MFCD22666388
• UNSPSCコード: 51111800
• PubChem Substance ID: 329823774
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 保管条件: desiccated
• 色: white to beige
• 溶解性: DMSO: 5 mg/mL (clear solution, warmed)
• 保管温度: room temp
• SMILES記法: 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

詳細

生物化学的／生理学的作用

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.

特徴および利点

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.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable