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Purity: ≥98%
GlyH-101 is a novel and potent CFTR inhibitor (cystic fibrosis transmembrane conductance regulator) with Ki of 1.4 uM. GlyH-101 is a glycine hydrazide that has been shown to block CFTR channels. 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). GlyH-101 blocks the open pore of cardiac CFTR channels at an electrical distance of 0.15 ± 0.03 from the external membrane surface.
| 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].
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| ln Vivo |
GlyH-101 (2.5 µg) decreases intestinal fluid secretion in mice caused by cholera toxin by about 80%[2].
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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. |
| References |
[1]. Muanprasat C, et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004 Aug;124(2):125-37.
[2]. Kelly M, et al. Cystic fibrosis transmembrane regulator inhibitors CFTR(inh)-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J Pharmacol Exp Ther. 2010 Apr;333(1):60-9. [3]. Barman PP, et al. Cardiac ion channel current modulation by the CFTR inhibitor GlyH-101. Biochem Biophys Res Commun. 2011 Apr 29;408(1):12-7. [4]. Melis N, et al. Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors. Br J Pharmacol. 2014 Aug;171(15):3716-27. [5]. Muanprasat C, et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004 Aug;124(2):125-37. |
| Molecular Formula |
C19H15BR2N3O3
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|---|---|
| Molecular Weight |
493.1487
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| CAS # |
328541-79-3
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| SMILES |
O=C(N/N=C/C1=C(O)C(Br)=C(O)C(Br)=C1)CNC2=CC3=CC=CC=C3C=C2
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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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| 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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