774549-97-2

774549-97-2 structure

Name: KM 11060
Chemical Name: 7-chloro-4-[4-(4-chlorophenyl)sulfonylpiperazin-1-yl]quinoline
CAS Number: 774549-97-2
Molecular Formula: C₁₉H₁₇Cl₂N₃O₂S
Molecular Weight: 422.328
Catalog: Signaling Pathways Membrane Transporter/Ion Channel CFTR
Create Date: 2018-11-26 15:35:48
Modify Date: 2024-01-24 17:48:34
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]

Name	7-chloro-4-[4-(4-chlorophenyl)sulfonylpiperazin-1-yl]quinoline
Synonyms	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

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.

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

98-60-2

837-52-5

~96%

774549-97-2

86-98-6

774549-97-2

Precursor 3
98-60-2 837-52-5 86-98-6
DownStream 0

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%