| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
In baby hamster kidney (BHK) cells, glafenine raises mutant CFTR's surface expression to 40% of that of wild-type CFTR [2]. In a dose-dependent manner, glafenineHCl suppresses the clonogenic activity and proliferation of EC and haSMC. Phase decrease and G2/M phase arrest take place. Tenascin, an extracellular matrix protein, is decreased and the migratory capacity of human stem cells (haSMCs) is hampered in a dose-dependent manner [3].
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| ln Vivo |
Mice administered a glafenine injection (25 mg/kg intraperitoneally) and the BLI signal improved; on average, the amplification was 2.9 times greater than the control. When compared to the signal generated by these xenografts before to injection, grafenine increased the BLI signal in two different HEK293/ABCG2/fLuc xenografts from the same mouse by up to 11.6 and 17.4 times, respectively [1]. Glaffenine treatment increases the responsiveness of polarized CFBE410-cell monolayers and the intestinal tracts isolated from mutant CFTR animals to forskolin and genistein in terms of short-circuit currents. Additionally, grafenine therapy partially restores full salivation [2]. Zebrafish treated with aflatoxin (glafenin) exhibited endoplasmic reticulum and mitochondrial stress, intestinal destruction, cessation of cellular stress responses, and an accumulation of apoptotic intestinal epithelial cells in the lumen [4].
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| References |
[1]. Zhang Y, et al. Identification of inhibitors of ABCG2 by a bioluminescence imaging-based high-throughput assay. Cancer Res. 2009 Jul 15;69(14):5867-75.
[2]. Robert R, et al. Correction of the Delta phe508 cystic fibrosis transmembrane conductance regulator trafficking defect by the bioavailable compound glafenine. Mol Pharmacol. 2010 Jun;77(6):922-30. [3]. Schöber W, et al. Impact of glafenine hydrochloride on human endothelial cells and human vascular smooth muscle cells: a substance reducing proliferation, migration and extracellular matrix synthesis. Cell Biol Int. 2003;27(12):987-96. [4]. Goldsmith JR, et al. Glafenine-induced intestinal injury in zebrafish is ameliorated by μ-opioid signaling via enhancement of Atf6-dependent cellular stress responses. Dis Model Mech. 2013 Jan;6(1):146-5 |
| Molecular Formula |
C19H18CL2N2O4
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|---|---|
| Molecular Weight |
409.2632
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| Exact Mass |
408.064
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| CAS # |
65513-72-6
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| Related CAS # |
Glafenine;3820-67-5
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| PubChem CID |
3085326
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
618ºC at 760 mmHg
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| Flash Point |
327.6ºC
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| LogP |
4.016
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
467
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C2C(C=1[H])=NC([H])=C([H])C=2N([H])C1=C([H])C([H])=C([H])C([H])=C1C(=O)OC([H])([H])C([H])(C([H])([H])O[H])O[H].Cl[H]
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| InChi Key |
CEUMONXVSJOJIH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17ClN2O4.ClH/c20-12-5-6-14-17(7-8-21-18(14)9-12)22-16-4-2-1-3-15(16)19(25)26-11-13(24)10-23;/h1-9,13,23-24H,10-11H2,(H,21,22);1H
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| Chemical Name |
2,3-dihydroxypropyl 2-[(7-chloroquinolin-4-yl)amino]benzoate;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~41.67 mg/mL (~101.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4434 mL | 12.2172 mL | 24.4343 mL | |
| 5 mM | 0.4887 mL | 2.4434 mL | 4.8869 mL | |
| 10 mM | 0.2443 mL | 1.2217 mL | 2.4434 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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