Synonym
KM11060; KM-11060; KM 11060.
IUPAC/Chemical Name
7-chloro-4-(4-((4-chlorophenyl)sulfonyl)piperazin-1-yl)quinoline
InChi Key
GIEHIZKCIZLXLF-UHFFFAOYSA-N
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
SMILES Code
O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C23)CC1)(C4=CC=C(Cl)C=C4)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
KM11060 is a corrector of the F508 deletion (F508del)-cystic fibrosis transmembrane conductance regulator (CFTR) trafficking defect.
In vitro activity:
By contrast, corrector KM11060 was a P-gp substrate as it stimulated P-gp ATPase activity and rescued the G268V mutant. Expression of wild-type P-gp reduced the effectiveness of CFTR rescue by corrector KM11060 by about 5-fold.
Reference: Biochem Pharmacol. 2012 Feb 1;83(3):345-54. https://pubmed.ncbi.nlm.nih.gov/22138447/
In vivo activity:
In LPS-induced acute lung inflammation, blockade of PSGL-1 (P-selectin glycoprotein ligand-1) or P-selectin, antagonism of PAF by WEB2086, or correction of mutated CFTR trafficking by KM11060 could significantly increase plasma lipoxin A4 levels in F508del relevant to wildtype mice.
Reference: PLoS One. 2014 Mar 26;9(3):e93003. https://pubmed.ncbi.nlm.nih.gov/24671173/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
5.0 |
11.84 |
| DMSO |
46.3 |
109.71 |
| Ethanol |
1.3 |
2.96 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
422.32
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Loo TW, Bartlett MC, Shi L, Clarke DM. Corrector-mediated rescue of misprocessed CFTR mutants can be reduced by the P-glycoprotein drug pump. Biochem Pharmacol. 2012 Feb 1;83(3):345-54. doi: 10.1016/j.bcp.2011.11.014. Epub 2011 Nov 28. PMID: 22138447.
2. Robert R, Carlile GW, Pavel C, Liu N, Anjos SM, Liao J, Luo Y, Zhang D, Thomas DY, Hanrahan JW. Structural analog of sildenafil identified as a novel corrector of the F508del-CFTR trafficking defect. Mol Pharmacol. 2008 Feb;73(2):478-89. doi: 10.1124/mol.107.040725. Epub 2007 Nov 1. PMID: 17975008.
3. Wu H, Yang J, Su EM, Li L, Zhao C, Yang X, Gao Z, Pan M, Sun P, Sun W, Jiang Y, Su X. 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. doi: 10.1371/journal.pone.0093003. PMID: 24671173; PMCID: PMC3966846.
In vitro protocol:
1. Loo TW, Bartlett MC, Shi L, Clarke DM. Corrector-mediated rescue of misprocessed CFTR mutants can be reduced by the P-glycoprotein drug pump. Biochem Pharmacol. 2012 Feb 1;83(3):345-54. doi: 10.1016/j.bcp.2011.11.014. Epub 2011 Nov 28. PMID: 22138447.
2. Robert R, Carlile GW, Pavel C, Liu N, Anjos SM, Liao J, Luo Y, Zhang D, Thomas DY, Hanrahan JW. Structural analog of sildenafil identified as a novel corrector of the F508del-CFTR trafficking defect. Mol Pharmacol. 2008 Feb;73(2):478-89. doi: 10.1124/mol.107.040725. Epub 2007 Nov 1. PMID: 17975008.
In vivo protocol:
1. Wu H, Yang J, Su EM, Li L, Zhao C, Yang X, Gao Z, Pan M, Sun P, Sun W, Jiang Y, Su X. 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. doi: 10.1371/journal.pone.0093003. PMID: 24671173; PMCID: PMC3966846.
1: Wu H, Yang J, Su EM, Li L, Zhao C, Yang X, Gao Z, Pan M, Sun P, Sun W, Jiang
Y, Su X. 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. doi: 10.1371/journal.pone.0093003. eCollection 2014. PubMed PMID:
24671173; PubMed Central PMCID: PMC3966846.
2: Loo TW, Bartlett MC, Shi L, Clarke DM. Corrector-mediated rescue of
misprocessed CFTR mutants can be reduced by the P-glycoprotein drug pump. Biochem
Pharmacol. 2012 Feb 1;83(3):345-54. doi: 10.1016/j.bcp.2011.11.014. Epub 2011 Nov
28. PubMed PMID: 22138447.
3: Robert R, Carlile GW, Pavel C, Liu N, Anjos SM, Liao J, Luo Y, Zhang D, Thomas
DY, Hanrahan JW. Structural analog of sildenafil identified as a novel corrector
of the F508del-CFTR trafficking defect. Mol Pharmacol. 2008 Feb;73(2):478-89.
Epub 2007 Nov 1. PubMed PMID: 17975008.
