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Purity: ≥98%
KM11060 is a novel mutated corrector of the F508del-CFTR (cystic fibrosis transmembrane conductance regulator) trafficking defect. It corrects F508del-CFTR trafficking, and increases the amount of functional CFTR at the plasma membrane (~75%) and inhibits PDE5 activity. Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing defect and in the development of cystic fibrosis therapeutics. KM11060 partially corrects F508del-CFTR processing and increases surface expression to 75% of that observed in cells incubated at low temperature. Up to 50% of the F508del-CFTR in cells treated with KM11060 was complex-glycosylated, indicating passage through the Golgi. KM11060 as a promising compound for further development of CF therapeutics.
| ln Vitro |
Pharmacological tools like KM11060, which are small-molecule correctors, could be beneficial in researching the F508del-CFTR processing problem and developing treatments for cystic fibrosis. In both native epithelial tissues and cultured cells, KM11060 restores F508del-CFTR trafficking. F508del-CFTR processing is largely corrected by KM11060, which also raises surface expression to 75% of what is seen in cells cultured at low temperature. In cells treated with KM11060, up to 50% of the F508del-CFTR was complex-glycosylated, indicating Golgi transit. KM11060 is a potentially useful substance for the advancement of CF treatments. [1]
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| ln Vivo |
When LPS causes acute lung inflammation, plasma lipoxin A4 levels in F508del mice relative to wildtype mice can be markedly elevated by blocking PSGL-1 (P-selectin glycoprotein ligand-1) or P-selectin, blocking PAF by WEB2086, or correcting mutated CFTR trafficking by KM11060. [2]
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| Enzyme Assay |
KM11060 is a novel corrector of the F508del-CFTR (cystic fibrosis transmembrane conductance regulator) trafficking defect. It corrects F508del-CFTR trafficking, and increases the amount of functional CFTR at the plasma membrane (~75%) and inhibits PDE5 activity.
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| Cell Assay |
Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing defect and in the development of cystic fibrosis therapeutics. KM11060 rescues F508del-CFTR trafficking in cultured cells and native epithelial tissues. KM11060 partially corrects F508del-CFTR processing and increases surface expression to 75% of that observed in cells incubated at low temperature. Up to 50% of the F508del-CFTR in cells treated with KM11060 was complex-glycosylated, indicating passage through the Golgi. KM11060 as a promising compound for further development of CF therapeutics.
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| Animal Protocol |
Mice
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| References |
[1]. Robert R, et al. Structural analog of sildenafil identified as a novel corrector of the F508del-CFTR trafficking defect. Mol Pharmacol. 2008 Feb;73(2):478-89.
[2]. Wu H, et al. Lipoxin A4 and platelet activating factor are involved in E. coli or LPS-induced lung inflammation in CFTR-deficient mice. PLoS One. 2014 Mar 26;9(3):e93003. |
| Molecular Formula |
C19H17CL2N3O2S
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| Molecular Weight |
422.33
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| Exact Mass |
421.0419
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| Elemental Analysis |
C, 54.04; H, 4.06; Cl, 16.79; N, 9.95; O, 7.58; S, 7.59
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| CAS # |
774549-97-2
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C23)CC1)(C4=CC=C(Cl)C=C4)=O
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| InChi Key |
GIEHIZKCIZLXLF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17Cl2N3O2S/c20-14-1-4-16(5-2-14)27(25,26)24-11-9-23(10-12-24)19-7-8-22-18-13-15(21)3-6-17(18)19/h1-8,13H,9-12H2
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| Chemical Name |
7-chloro-4-(4-((4-chlorophenyl)sulfonyl)piperazin-1-yl)quinoline
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| Synonyms |
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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 |
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| 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: ~84 mg/mL ( 198.89 mM）
Water: Insoluble Ethanol: <2 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10%DMSO+90%corn oil：≥ 5 mg/mL (11.84 mM); Clear solution (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3678 mL | 11.8391 mL | 23.6782 mL | |
| 5 mM | 0.4736 mL | 2.3678 mL | 4.7356 mL | |
| 10 mM | 0.2368 mL | 1.1839 mL | 2.3678 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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