219671

GlyH-101

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

• Synonym(e): CFTR-Inhibitor II, GlyH-101
• Empirische Formel (Hill-System): C₁₉H₁₅Br₂N₃O₃
• CAS-Nummer: 328541-79-3
• Molekulargewicht: 493.15
• MDL number: MFCD01532954
• UNSPSC Code: 12352200
• NACRES: NA.28
• Assay: ≥97% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze

Eigenschaften

• Produktname: 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).
• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: yellow
• solubility: DMSO: 200 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: 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

Beschreibung

General description

Eine zellpermeable Glycinylhydrazon-Verbindung, die als potenter, selektiver und reversibler offener Kanal-Blocker von CFTR mit einer mittleren Geschwindigkeit dient (<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).

Biochem/physiol Actions

Primärziel
CFTR

Produkt konkurriert nicht mit ATP.

Reversibel: ja

Zellpermeabel: ja

Ziel-IC₅₀: 95%ige Hemmung bei 50 µmol/l

Ziel-K_i: 4,3 µmol/l in CFTR-exprimierenden FRT-Zellen für den Cl−-Strom der apikalen Membran

Preparation Note

Nach der Rekonstitution in Aliquote aufteilen und einfrieren (-20 °C). Stammlösungen sind bei -20 °C bis zu 3 Monate haltbar.

Other Notes

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

Legal Information

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

Disclaimer

Toxizität: Standard-Handhabung (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable