1. Membrane Transporter/Ion Channel
  2. CFTR
  3. GlyH-101

GlyH-101 

Cat. No.: HY-18336 Purity: 99.0%
Handling Instructions

GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.

For research use only. We do not sell to patients.

GlyH-101 Chemical Structure

GlyH-101 Chemical Structure

CAS No. : 328541-79-3

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Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 106 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 624 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GlyH-101 purchased from MCE. Usage Cited in: Sci Rep. 2018 Apr 16;8(1):6028.

    Western blot analysis of expression and phosphorylation of H3 in GlyH-101 (10 nM for 48 hours)-treated cells.
    • Biological Activity

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    Description

    GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM. IC50 value: 1.4 uM (Ki, at +60 mV) [1] Target: CFTR in vitro: GlyH-101 reversibly inhibited CFTR Cl- conductance in <1 min. Whole-cell current measurements revealed voltage-dependent CFTR block by GlyH-101 with strong inward rectification, producing an increase in apparent inhibitory constant Ki from 1.4 microM at +60 mV to 5.6 microM at -60 mV. GlyH-101 inhibitory potency was independent of pH from 6.5-8.0, where it exists predominantly as a monovalent anion with solubility approximately 1 mM in water[1]. In HeLa cells, these events were associated with a decrease in the rate of oxygen consumption, with GlyH-101 demonstrating a higher potency than CFTR(inh)-172. The impact of CFTR inhibitors on inflammatory parameters was also tested in HeLa cells. CFTR(inh)-172, but not GlyH-101, induced nuclear translocation of nuclear factor-kappaB (NF-kappaB) [2]. GlyH-101 is a glycine hydrazide that has recently been shown to block CFTR channels but its effects on cardiomyocytes are unknown. Here the action of GlyH-101 on cardiac I(Cl.PKA) and on other ion currents has been established. Whole-cell patch-clamp recordings were made from rabbit isolated ventricular myocytes. GlyH-101 blocked I(Cl.PKA) in a concentration- and voltage-dependent fashion (IC(50) at +100 mV=0.3 ± 1.5 μM and at -100 mV=5.1 ± 1.3 μM) [3]. in vivo: Topical GlyH-101 (10 microM) in mice rapidly and reversibly inhibited forskolin-induced hyperpolarization in nasal potential differences. In a closed-loop model of cholera, intraluminal GlyH-101 (2.5 microg) reduced by approximately 80% cholera toxin-induced intestinal fluid secretion [1].

    Molecular Weight

    493.15

    Formula

    C₁₉H₁₅Br₂N₃O₃

    CAS No.
    SMILES

    O=C(N/N=C/C1=CC(Br)=C(O)C(Br)=C1O)CNC2=CC3=CC=CC=C3C=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 58 mg/mL (117.61 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0278 mL 10.1389 mL 20.2778 mL
    5 mM 0.4056 mL 2.0278 mL 4.0556 mL
    10 mM 0.2028 mL 1.0139 mL 2.0278 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    GlyH-101GlyH101GlyH 101CFTRCystic fibrosis transmembrane conductance regulatorInhibitorinhibitorinhibit

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    Product Name:
    GlyH-101
    Cat. No.:
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