A reversible CFTR channel blocker
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

CFTR Inhibitor II

Item No. 15772

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3,5-dibromo-2,4-dihydroxyphenyl)methylene]hydrazide N-2-naphthalenyl-glycine
CAS Number
328541-79-3
Synonyms
  • GlyH-101
  • Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor II
Molecular Formula
C19H15Br2N3O3
Formula Weight
493.2
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 25 mg/ml
λmax
243, 289, 329 nm
SMILES
O=C(N/N=C/C1=C(O)C(Br)=C(O)C(Br)=C1)CNC2=CC3=CC=CC=C3C=C2
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $46

    Add

    10 mg

    $81

    Add

    25 mg

    $157

    Add

    50 mg

    $290

    Add
    Cayman Chemical
    Neutrophil Biology Wall Poster

    Explore how neutrophils shape the immune response in health and disease. This poster highlights neutrophil pathogen defense mechanisms, including phagocytosis, degranulation, and NETosis, as well as neutrophil roles in inflammation and NET-associated pathologies.

    DOWNLOAD NOW
    Product Description

    The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR).1 CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 µM).2,3 This compound binds to a site at the external pore of CFTR, occluding the pore and rapidly preventing chloride transport.2,3 Intraluminal CFTR inhibitor II greatly reduces intestinal fluid secretion induced by cholera toxin.3 It is effective in cells in culture and also in nasal and intestinal epithelia in vivo.4,5,6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Derand, R., Bulteau-Pignoux, L., and Becq, F. The cystic fibrosis mutation G551D alters the non-Michaelis-Menten behavior of the cystic fibrosis transmembrane conductance regulator (CFTR) channel and abolishes the inhibitory genistein binding site. The Journal of Biological Chemisty 277(39), 35999-36004 (2002).

    2. Sonawane, N.D., Hu, J., Muanprasat, C., et al. Luminally active, nonabsorbable CFTR inhibitors as potential therapy to reduce intestinal fluid loss in cholera. FASEB J. 20(1), 130-132 (2006).

    3. Muanprasat, C., Sonawane, N.D., Salinas, D., et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: Mechanism, structure-activity analysis, and in vivo efficacy. J. Gen. Physiol. 124(2), 125-137 (2004).

    4. MacVinish, L.J., Cope, G., Ropenga, A., et al. Chloride transporting capability of Calu-3 epithelia following persistent knockdown of the cystic fibrosis transmembrane conductance regulator, CFTR. Br. J. Pharmacol. 150(8), 1055-1065 (2007).

    5. Garnett, J.P., Hickman, E., Tunkamnerdthai, O., et al. Protein phosphatase 1 coordinates CFTR-dependent airway epithelial HCO3- secretion by reciprocal regulation of apical and basolateral membrane Cl--HCO3- exchangers. Br. J. Pharmacol. 168(8), 1946-1960 (2013).

    6. Schiffhauer, E.S., Vij, N., Kovbasnjuk, O., et al. Dual activation of CFTR and CLCN2 by lubiprostone in murine nasal epithelia. Am. J. Physiol. Lung Cell. Mol. Physiol. 304(5), L324-L331 (2013).

    7. Zertal-Zidani, S., Busiah, K., Edelman, A., et al. Small-molecule inhibitors of the cystic fibrosis transmembrane conductance regulator increase pancreatic endocrine cell development in rat and mouse. Diabetologia 56(2), 330-339 (2013).