KM 11060

Names

[ Name ]:
KM 11060

[Synonym ]:
7-Chloro-4-{4-[(4-chlorophenyl)sulfonyl]-1-piperazinyl}quinoline
Quinoline, 7-chloro-4-[4-[(4-chlorophenyl)sulfonyl]-1-piperazinyl]-
7-chloro-4-{4-[(4-chlorophenyl)sulfonyl]piperazin-1-yl}quinoline
7-chloro-4-{4-[(4-chlorophenyl)sulfonyl]piperazino}quinoline
KM 11060
KM11060

Biological Activity

[Description]:

KM11060 is a novel corrector of the F508del-CFTR trafficking defect.Target: CFTRin vitro: 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. [1]in vivo: 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. [2]

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR

Research Areas >> Endocrinology

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
607.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₇Cl₂N₃O₂S

[ Molecular Weight ]:
422.328

[ Flash Point ]:
321.1±34.3 °C

[ Exact Mass ]:
421.041840

[ PSA ]:
61.89000

[ LogP ]:
4.19

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.676

[ Storage condition ]:
2-8℃

MSDS

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Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Personal Protective Equipment ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ RIDADR ]:
UN 2811 6.1 / PGIII

[ HS Code ]:
2935009090

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

Articles

Important role of platelets in modulating endotoxin-induced lung inflammation in CFTR-deficient mice.

PLoS ONE 8 , e82683, (2013)

Mutation of CFTR (cystic fibrosis transmembrane conductance regulator) leads to cystic fibrosis (CF). Patients with CF develop abnormalities of blood platelets and recurrent lung inflammation. However...