| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GlyH-101 targets the CFTR chloride channel, a cAMP-regulated anion channel that is essential for epithelial fluid secretion and ion transport. As a reversible open-channel blocker, GlyH-101 binds to the open state of the CFTR channel and physically occludes the pore, preventing chloride ion flux. The compound has a Ki of 4.3 µM in CFTR-expressing FRT cells. It inhibits CFTR Cl⁻ conductance in <1 min.
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| ln Vitro |
In PCT and PS120 cells, GlyH-101 (0-50 µM) demonstrates anti-proliferative action [1]. PCT cells' CFTR-like currents are inhibited by GlyH-101 (0.5, 1, 5, 10 µM) in a concentration-dependent manner [1]. VSORC current is inhibited by GlyH-101 (0.5, 1, 5, 10 µM), having IC50 values of 5.38 and 6.26 µM for PS120 and PCT cells, respectively [1].
GlyH-101 inhibits CFTR chloride conductance in <1 minute. In rabbit isolated ventricular myocytes, this compound also blocks cardiac I(Cl.PKA) channels. In transfected FRT (SLC26A9-FRT) cells, GlyH-101 inhibits CFTR activity. The compound's inhibition is voltage-dependent. Its activity can be assessed using patch-clamp electrophysiology or using iodide efflux assays in CFTR-expressing cells. |
| ln Vivo |
GlyH-101 (2.5 µg) decreases intestinal fluid secretion in mice caused by cholera toxin by about 80%[2].
GlyH-101 is used in vivo in research to study CFTR function, epithelial fluid secretion, and ion transport physiology. It is widely used as a research tool to investigate the role of CFTR in various physiological and pathological processes, including cystic fibrosis, cholera, and other diseases involving epithelial ion transport. |
| Enzyme Assay |
Non-cellular enzyme assays for GlyH-101 are limited as it acts on an ion channel rather than through enzyme inhibition. Its binding affinity for the CFTR channel can be assessed using radioligand binding studies with membrane preparations from cells expressing CFTR. The compound's physicochemical properties can be characterized using standard analytical techniques.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PCT, PS120 Cell Tested Concentrations: 0, 1, 5, 10, 20, 50 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cell growth in a dose-dependent manner. In vitro cellular assays for GlyH-101 involve treating CFTR-expressing cells with the compound and measuring chloride channel activity. Patch-clamp electrophysiology is used to assess the inhibition of CFTR-mediated chloride currents. Alternatively, iodide efflux assays can be used, where cells are loaded with iodide and the efflux of iodide through CFTR channels is measured in the presence of varying concentrations of GlyH-101. The Ki for CFTR inhibition is determined from dose-response curves. |
| Animal Protocol |
In vivo animal experiments with GlyH-101 are conducted in animal models to study CFTR function and epithelial fluid secretion. The compound is administered via various routes, and its effects on fluid secretion in tissues such as the airways, intestine, and sweat glands are assessed. GlyH-101 has been used in studies across evolutionarily distant species, including shark and pig.
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| ADME/Pharmacokinetics |
GlyH-101 has a molecular weight of 493.15 and a molecular formula of C19H15Br2N3O3. It is a solid at room temperature with a purity of ≥97%. The compound is soluble in DMSO and other organic solvents. It is typically stored at -20°C. GlyH-101 is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
GlyH-101 is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. Appropriate personal protective equipment should be used.
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| References |
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| Additional Infomation |
Glycine, n-2-naphthyl-,2-[(3,5-dibromo-2,4-dihydroxyphenyl)methylene] hydrazide is a member of the naphthalene family of compounds.
GlyH-101 (CFTR Inhibitor II; CAS 328541-79-3) is a cell-permeable, potent, selective, and reversible open-channel blocker of the CFTR chloride channel. It has a Ki of 4.3 µM in CFTR-expressing FRT cells. GlyH-101 is widely used in research to study CFTR function, epithelial fluid secretion, and ion transport physiology. The compound is available from various commercial suppliers for research applications. |
| Molecular Formula |
C19H15BR2N3O3
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|---|---|
| Molecular Weight |
493.1487
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| Exact Mass |
490.947
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| CAS # |
328541-79-3
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| PubChem CID |
135476586
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.696
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| LogP |
6.92
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C=C(C=CC2=C1)NCC(=O)N/N=C/C3=CC(=C(C(=C3O)Br)O)Br
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| InChi Key |
RMBDLOATEPYBSI-NUGSKGIGSA-N
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| 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+
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| Synonyms |
GlyH101 GlyH 101 GlyH-101.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 58 mg/mL (~117.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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