PZ0319

PF-06409577

≥98% (HPLC)

• 同義詞: 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid
• 經驗公式（希爾表示法）: C₁₉H₁₆ClNO₃
• CAS號碼: 1467057-23-3
• 分子量：: 341.79
• 分類程式碼代碼: 12352200
• PubChem物質ID: 329823837
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: white to beige
• 溶解度: DMSO: 20 mg/mL, clear
• 儲存溫度: room temp
• SMILES 字串: 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 密鑰: FHQXLWCFSUSXBF-UHFFFAOYSA-N

描述

一般說明

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

應用

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

生化／生理作用

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.

安全資訊

• 象形圖: GHS07
• 訊號詞: Warning
• 危險聲明: H315,H319,H335
• 防範說明: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• 危險分類: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• 標靶器官: Respiratory system
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable