219671

GlyH-101

≥97% (HPLC), solid, CFTR inhibitor, Calbiochem^®

• 別名: CFTR Inhibitor II, GlyH-101, N-(2-Naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide
• 実験式（ヒル表記法）: C₁₉H₁₅Br₂N₃O₃
• CAS番号: 328541-79-3
• 分子量: 493.15
• MDL番号: MFCD01532954
• UNSPSCコード: 12352200
• NACRES: NA.28

特性

• 製品名: CFTR Inhibitor II, GlyH-101, CFTR Inhibitor II, GlyH-101, CAS 328541-79-3, is a cell-permeable potent, selective and reversible open-channel blocker of CFTR (K_i = 4.3 µM in CFTR-expressing FRT cells).
• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: yellow
• 溶解性: DMSO: 200 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: Brc1c(c(cc(c1O)\C=N\NC(=O)CNc2cc3c(cc2)cccc3)Br)O
• InChI: 1S/C19H15Br2N3O3/c20-15-8-13(18(26)17(21)19(15)27)9-23-24-16(25)10-22-14-6-5-11-3-1-2-4-12(11)7-14/h1-9,22,26-27H,10H2,(H,24,25)/b23-9+
• InChI Key: RMBDLOATEPYBSI-NUGSKGIGSA-N

詳細

詳細

A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (<1 min; 95% inhibition at 50 µM; K_i = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl^- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl^- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl^- currents, and is effective in nasal and intestinal epithelia in vivo.

A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (<1 min; 95% inhibition at 50 µM; K_i = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl^- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl^- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl^- currents, and is effective in nasal and intestinal epithelia in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 219675).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
CFTR

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 95% inhibition at 50 µM

Target K_i: 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Sonawane, N.D., et al. 2006. FASEB J.20, 130.
Muanprasat, C., et al. 2004. J. Gen. Physiol.124, 125.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable