Skip to Content
Merck
All Photos(1)

Key Documents

219671

Sigma-Aldrich

GlyH-101

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

Synonym(s):

CFTR Inhibitor II, GlyH-101, N-(2-Naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C19H15Br2N3O3
CAS Number:
328541-79-3
Molecular Weight:
493.15
UNSPSC Code:
12352200
NACRES:
NA.28

product name

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 (Ki = 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

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

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; Ki = 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; Ki = 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

Cell permeable: yes
Primary Target
CFTR
Product does not compete with ATP.
Reversible: yes
Target IC50: 95% inhibition at 50 µM
Target Ki: 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Amnah Yamani et al.
Mucosal immunology, 14(1), 135-143 (2020-06-25)
Food-triggered anaphylaxis can encompass a variety of systemic and intestinal symptoms. Murine-based and clinical studies have revealed a role for histamine and H1R and H2R-pathway in the systemic response; however, the molecular processes that regulate the gastrointestinal (GI) response are
R K Dutta et al.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 142, 112090-112090 (2021-09-01)
MicroRNAs play an important role in health and disease. TGF-β signaling, upregulated by HIV Tat, and in chronic airway diseases and smokers upregulates miR-145-5p to suppress cystic fibrosis transmembrane conductance regulator (CFTR). CFTR suppression in chronic airway diseases like Cystic
Juliette L Simonin et al.
Cells, 11(9) (2022-05-15)
Defective hydration of airway surface mucosa is associated with recurrent lung infection in cystic fibrosis (CF), a disease caused by CF transmembrane conductance regulator (CFTR) gene mutations. Whether the composition and/or presence of an airway surface liquid (ASL) is sufficient
Barbara Calabrese et al.
Nature communications, 13(1), 6037-6037 (2022-10-14)
During early ischemic brain injury, glutamate receptor hyperactivation mediates neuronal death via osmotic cell swelling. Here we show that ischemia and excess NMDA receptor activation cause actin to rapidly and extensively reorganize within the somatodendritic compartment. Normally, F-actin is concentrated

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service