PZ0319

PF-06409577

≥98% (HPLC)

• 別名: 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid
• 実験式（ヒル表記法）: C₁₉H₁₆ClNO₃
• CAS番号: 1467057-23-3
• 分子量: 341.79
• UNSPSCコード: 12352200
• PubChem Substance ID: 329823837
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 20 mg/mL, clear
• 保管温度: room temp
• SMILES記法: ClC1=C(C2=CC=C(C3(O)CCC3)C=C2)C=C4C(NC=C4C(O)=O)=C1
• InChI: 1S/C19H16ClNO3/c20-16-9-17-14(15(10-21-17)18(22)23)8-13(16)11-2-4-12(5-3-11)19(24)6-1-7-19/h2-5,8-10,21,24H,1,6-7H2,(H,22,23)
• InChI Key: FHQXLWCFSUSXBF-UHFFFAOYSA-N

詳細

詳細

PF-06409577 is a 6-chloro-indole derivative obtained from 5-bromo-6-chloro-indole.

アプリケーション

PF-06409577 has been used to determine its potential as a therapeutic agent for diabetic nephropathy.

生物化学的／生理学的作用

PF-06409577 is a potent and selective activator of 5′ adenosine monophosphate-activated protein kinase (AMPK).

PF-06409577 potently activates a1β1γ1 AMPK (5′ adenosine monophosphate-activated protein kinase) isoform, and prevents its dephosphorylation. It is similarly potent for β1 containing isoforms, but shows significantly lower potency for β2-containing isoforms of AMPK. Patch-clamp assays show that this compound does not inhibit hERG (human ether-a-go-go gene). It interacts with the allosteric drug and metabolite site (ADaM) of AMPK.

PF-06409577 preserves retinal pigment epithelium cells from UV radiation by activating AMPK (AMP-activated protein kinase) signaling. This orally bioavailable and possesses pharmacokinetic properties. PF-06409577 blocks de novo lipid and cholesterol synthesis pathways that shows a decrease in hepatic lipids and mRNA expression of markers of hepatic fibrosis.

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H315,H319,H335
• 注意書き: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• 危険有害性の分類: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• ターゲットの組織: Respiratory system
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable