SML0774

SR 3677

≥98% (HPLC)

• 別名: N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide., SR-3677, SR3677
• 実験式（ヒル表記法）: C₂₂H₂₄N₄O₄
• CAS番号: 1072959-67-1
• 分子量: 408.45
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to light brown
• 溶解性: DMSO: 15 mg/mL, clear
• 保管温度: 2-8°C
• InChI: 1S/C22H24N4O4/c1-26(2)9-10-28-20-11-15(16-12-23-24-13-16)7-8-17(20)25-22(27)21-14-29-18-5-3-4-6-19(18)30-21/h3-8,11-13,21H,9-10,14H2,1-2H3,(H,23,24)(H,25,27)
• InChI Key: OQWZIAVXCYIZNN-UHFFFAOYSA-N

詳細

アプリケーション

SR 3677 has been used as Rho-associated kinase (ROCK) inhibitor in cardiac reprogramming.[1]

生物化学的／生理学的作用

SR-3677 is a very potent, selective ROCK inhibitor, with higher potency against ROCK II (IC₅₀ = 3 nM) than ROCK I (IC₅₀ = 56 nM). In a kinase screening panel, SR-3677 was shown to only have activity against three other kinases (PKA, MRCK and Akt1) all with IC₅₀ values over 1 μM. The compound has nM potency in cell based assays, and is efficacious in an ex-vivo model for increasing aqueous humor outflow in porcine eyes.

SR-3677 is a very potent, selective ROCK inhibitor.

SR3677 decreases amyloid precursor protein (sAPPβ) and amyloid-β (Aβ) in a dose-dependent manner. In 5XFAD mouse brain, SR3677 represses the enzymatic activity of β-site APP cleaving enzyme 1 (BACE1). SR3677 has the ability to change the endocytic supply of BACE1 and induce APP traffic to lysosomes.[2]

特徴および利点

This compound is featured on the PKA & PKG and PKB/Akt pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

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