SML0524

ML277

≥98% (HPLC)

• 別名: (2R)-N-[4-(4-Methoxyphenyl)-1,3-thiazol-2-yl]-1-(4-methylphenyl)sulfonylpiperidine-2-carboxamide, (R)-N-(4-(4-Methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, CID-53347902, VU0458298-2, VU0458298-3
• 実験式（ヒル表記法）: C₂₃H₂₅N₃O₄S₂
• CAS番号: 1401242-74-7
• 分子量: 471.59
• MDL番号: MFCD23704792
• UNSPSCコード: 12352200
• PubChem Substance ID: 329825530
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 5 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: COc1ccc(cc1)-c2cnc(NC(=O)[C@H]3CCCCN3S(=O)(=O)c4ccc(C)cc4)s2
• InChI: 1S/C23H25N3O4S2/c1-16-6-12-19(13-7-16)32(28,29)26-14-4-3-5-20(26)22(27)25-23-24-15-21(31-23)17-8-10-18(30-2)11-9-17/h6-13,15,20H,3-5,14H2,1-2H3,(H,24,25,27)/t20-/m1/s1
• InChI Key: UKSXJENCMIVQMU-HXUWFJFHSA-N

詳細

アプリケーション

ML277 has been used as the KCNQ1 activator to treat cells in lung metastasis assay.

生物化学的／生理学的作用

ML277 is a potent activator of KCNQ1 (Kv7.1) channels with >100-fold selectivity versus KCNQ2 and KCNQ4 and no activity against the hERG potassium channel up to 30 μM. KCNQ1 is a voltage-gated potassium channel required for repolarization phase of the cardiac action potential. Mutations in the KCNQ1 gene are associated with long QT syndrome (LQTS), a disorder in which the heart muscles take longer than normal to recover after each heart beat and can lead to dangerous arrhythmias such as atrial fibrillation. Activators of KCNQ1 channels could have potential use in treatments of LQTS. ML277 is the first selective and potent activator found, with an EC₅₀ of 260 nM.

特徴および利点

This compound is featured on the Potassium Channels page 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: H302,H319
• 注意書き: P264 - P270 - P280 - P301 + P312 - P305 + P351 + P338 - P337 + P313
• 危険有害性の分類: Acute Tox. 4 Oral - Eye Irrit. 2
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable