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Chemical Structure| 328541-79-3 Chemical Structure| 328541-79-3

Structure of GlyH-101
CAS No.: 328541-79-3

Chemical Structure| 328541-79-3

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GlyH-101, a glycinyl hydrazone compound, is a reversible and voltage-dependent CFTR chloride channel blocker with Ki of 4.3 μM.

Synonyms: CFTR Inhibitor II; Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor II

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Product Details of GlyH-101

CAS No. :328541-79-3
Formula : C19H15Br2N3O3
M.W : 493.15
SMILES Code : O=C(N/N=C/C1=CC(Br)=C(O)C(Br)=C1O)CNC2=CC=C3C=CC=CC3=C2
Synonyms :
CFTR Inhibitor II; Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor II
MDL No. :MFCD01532954
InChI Key :RMBDLOATEPYBSI-NUGSKGIGSA-N
Pubchem ID :135476586

Safety of GlyH-101

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • CFTR

    CFTR, Ki:4.3 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat pancreatic explants 10 μmol/l 1-7 days GlyH-101 increased the absolute number of NGN3+ endocrine progenitors and the number of beta cells, as well as the expression of insulin and Mafa. PMC3536988
Murine renal proximal convoluted tubule cells (PCT) 10 µM GlyH-101 blocked more than 70% of the CaCC conductance at 10 µM. PMC4128068
PS120 cells (non-CFTR expressing) 0.5, 1, 5, 10 µM GlyH-101 significantly inhibited VSORC currents with IC50 values of approximately 5.38 µM (negative potentials) and 6.26 µM (positive potentials). PMC4128068
Murine renal distal convoluted tubule cells (DCT) 0.5, 1, 5, 10 µM GlyH-101 induced a concentration-dependent inhibition of the CFTR-like current, with almost complete inhibition at 10 µM and a more pronounced effect at positive potentials. PMC4128068
Mouse beta-cells 50 μM 10 minutes To investigate the effect of GlyH-101 on cAMP-enhanced insulin secretion, results showed that GlyH-101 significantly inhibited cAMP-enhanced insulin secretion. PMC4035698
Human beta-cells 50 μM 10 minutes To investigate the effect of GlyH-101 on cAMP-enhanced insulin secretion, results showed that GlyH-101 significantly inhibited cAMP-enhanced insulin secretion. PMC4035698
Calu-3KD cells 50 μM 30 minutes GlyH-101 partially inhibited CFTR channel activity in Calu-3KD cells, but responses to lubiprostone and CCh were retained. PMC2013912
Calu-3WT cells 50 μM 30 minutes GlyH-101 completely inhibited CFTR channel activity in Calu-3WT cells, resulting in no response to lubiprostone or CCh. PMC2013912
Human airway smooth-muscle cells 2 μM 5 hours To evaluate the effects of GlyH-101 on cellular sphingolipid composition. Results showed GlyH-101 increased sphinganine and dihydroceramides. PMC7605160
Human alveolar epithelial cell line A549 2 μM 5 hours To evaluate the effects of GlyH-101 on cellular sphingolipid composition. Results showed GlyH-101 increased sphinganine and dihydroceramides. PMC7605160
Calu-3 cells 10 μM GlyH-101 had no effect on the mean alkalinization produced by the removal of basolateral Cl- under non-stimulated conditions, but in the presence of GlyH-101, the cAMP agonist forskolin failed to fully inhibit the basolateral exchanger PMC3623064
Normal Human Bronchial Epithelial cells (NHBE) 10 μM 20-50 minutes GlyH-101 significantly blocked H2O2-induced CFTR-dependent current changes PMC3824048

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Pregnant E12.5 mice Subcutaneous injection 10 mg/kg Twice daily for six consecutive days GlyH-101 increased the surface area of insulin+ and glucagon+ cells in E18.5 pancreases but did not modify beta cell proliferation. PMC3536988
Mice SPT-deficient mice Intratracheal administration 80 mg/kg Single dose, evaluated after 4 hours To evaluate the effects of GlyH-101 on airway hyperreactivity. Results showed GlyH-101 decreased AHR in SPT-deficient mice. PMC7605160

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.14mL

2.03mL

1.01mL

20.28mL

4.06mL

2.03mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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