KM 11060

Modify Date: 2024-01-24 17:48:34

KM 11060 Structure
KM 11060 structure
Common Name KM 11060
CAS Number 774549-97-2 Molecular Weight 422.328
Density 1.5±0.1 g/cm3 Boiling Point 607.3±65.0 °C at 760 mmHg
Molecular Formula C19H17Cl2N3O2S Melting Point N/A
MSDS Chinese USA Flash Point 321.1±34.3 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of KM 11060


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]

 Names

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

 KM 11060 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
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.

 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℃

 Safety Information

Symbol GHS06
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

 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%

 Articles1

More 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...

 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