KM 11060

Corrects F508del-CFTR trafficking CAS# 774549-97-2

KM 11060

Catalog No. BCC7578----Order now to get a substantial discount!

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KM 11060: 5mg $81 In Stock
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Chemical structure

KM 11060

3D structure

Chemical Properties of KM 11060

Cas No. 774549-97-2 SDF Download SDF
PubChem ID 1241327 Appearance Powder
Formula C19H17Cl2N3O2S M.Wt 422.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 10 mM in ethanol
Chemical Name 7-chloro-4-[4-(4-chlorophenyl)sulfonylpiperazin-1-yl]quinoline
SMILES C1CN(CCN1C2=C3C=CC(=CC3=NC=C2)Cl)S(=O)(=O)C4=CC=C(C=C4)Cl
Standard InChIKey GIEHIZKCIZLXLF-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of KM 11060

DescriptionCorrects F508del-CFTR trafficking; increases the amount of functional CFTR at the plasma membrane (~75%). Shown to inhibit PDE5 activity.

KM 11060 Dilution Calculator

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KM 11060 Molarity Calculator

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Preparing Stock Solutions of KM 11060

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3678 mL 11.8391 mL 23.6782 mL 47.3563 mL 59.1954 mL
5 mM 0.4736 mL 2.3678 mL 4.7356 mL 9.4713 mL 11.8391 mL
10 mM 0.2368 mL 1.1839 mL 2.3678 mL 4.7356 mL 5.9195 mL
50 mM 0.0474 mL 0.2368 mL 0.4736 mL 0.9471 mL 1.1839 mL
100 mM 0.0237 mL 0.1184 mL 0.2368 mL 0.4736 mL 0.592 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on KM 11060

KM11060 is a novel corrector of the F508del-CFTR trafficking defect. Target: CFTR in 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]

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.

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References on KM 11060

Osteobiographic analysis of skeleton I, Sitio Toca dos Coqueiros, Serra da Capivara National Park, Brazil, 11,060 BP: first results.[Pubmed:12012362]

Am J Phys Anthropol. 2002 Jun;118(2):99-110.

This paper presents an osteobiographic analysis of a single skeleton found in a small rock shelter known as Toca dos Coqueiros, Piaui, Brazil. This find is of interest because of an exceptionally old radiocarbon date associated with it. The date (11,060 BP) was obtained from charcoal associated directly with the skeleton. This is an interesting find because of the rarity of osteobiographic studies of skeletons of such antiquity. Despite the existence of two projectile points in association with the burial, the morphological and molecular analyses of the skeleton demonstrated that this was a female. She was about 35-45 years of age at death. The skeleton exhibited acute and chronic bone lesions. Oral pathology was also observed, including an interproximal dental groove, probably caused by the therapeutic use of a cactus thorn. This could be one of the oldest cases of an analgesic plant used in the prehistoric Americas.

Structural analog of sildenafil identified as a novel corrector of the F508del-CFTR trafficking defect.[Pubmed:17975008]

Mol Pharmacol. 2008 Feb;73(2):478-89.

The F508del mutation impairs trafficking of the cystic fibrosis transmembrane conductance regulator (CFTR) to the plasma membrane and results in a partially functional chloride channel that is retained in the endoplasmic reticulum and degraded. We recently used a novel high-throughput screening (HTS) assay to identify small-molecule correctors of F508del CFTR trafficking and found several classes of hits in a screen of 2000 compounds (Carlile et al., 2007). In the present study, we have extended the screen to 42,000 compounds and confirmed sildenafil as a corrector using this assay. We evaluated structural analogs of sildenafil and found that one such molecule called KM11060 (7-chloro-4-{4-[(4-chlorophenyl) sulfonyl] piperazino}quinoline) was surprisingly potent. It partially restored F508del trafficking and increased maturation significantly when baby hamster kidney (BHK) cells were treated with 10 nM for 24 h or 10 muM for 2 h. Partial correction was confirmed by the appearance of mature CFTR in Western blots and by using halide flux, patch-clamp, and short-circuit current measurements in unpolarized BHK cells, monolayers of human airway epithelial cells (CFBE41o(-)), and intestines isolated from F508del-CFTR mice (Cftr(tm1Eur)) treated ex vivo. 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.

Description

KM11060 is a novel corrector of the F508del-CFTR trafficking defect.

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