219675

CFTR Inhibitor II, GlyH-101

InSolution, ≥97%, potent, selective and reversible open-channel blocker of CFTR

• Synonym(s): InSolution CFTR Inhibitor II, GlyH-101, N-(2-Naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide
• Empirical Formula (Hill Notation): C₁₉H₁₅Br₂N₃O₃
• CAS Number: 328541-79-3
• Molecular Weight: 493.15
• MDL number: MFCD01532954
• UNSPSC Code: 12352200
• NACRES: NA.28
• Assay: ≥97% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

Properties

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: liquid
• potency: 4.3 μM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
• shipped in: dry ice
• storage temp.: −70°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

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

Packaging

Packaged under inert gas

Physical form

A 25 mM (5 mg/406 µL) solution of CFTR Inhibitor II, GlyH-101 (Cat. No. 219671) in DMSO.

Preparation Note

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 3 months at -70°C.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk: WGK 1
• flash_point_f: 188.6 °F - closed cup - (refers to pure substance)
• flash_point_c: 87 °C - closed cup - (refers to pure substance)