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Ko 143

Name: Ko 143
Brand: TargetMol
SKU: TQ0186
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0186Cas No. 461054-93-3

Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).

Ko 143

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Purity: 99.89%

Catalog No. TQ0186Cas No. 461054-93-3

Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$39	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$113	In Stock	In Stock
25 mg	$228	In Stock	In Stock
50 mg	$413	-	In Stock
100 mg	$745	-	In Stock
1 mL x 10 mM (in DMSO)	$66	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.89%

Appearance:Solid

Color:White to Green

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).
Targets&IC50	ABCG2:26 nM (EC50)
In vitro	In HEK G2 cells and mouse G2 cells, Ko143 (10 nM) significantly decreases the IC50 of MTX. Ko143 (1-100 μM) metabolite does not inhibit the function of ABC transporters [1]. Reversal of drug resistance in SKF 104864A-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by Ko143 [2]. Ko143 inhibits BCRP-mediated transport of ZD 4522 in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells [3].
In vivo	Ko143 (10 mg/kg, p.o.) increases the oral availability of SKF 104864A in mice [2].
Cell Research	Cells are plated at 400 or 1000/well in 96-well plates the night before the addition of drugs. A concentration series of the drug is applied along one plate axis and left for the duration of the assay. Plates are harvested after 4-5 days while untreated wells are still subconfluent. Relative cell proliferation is quantified with CyQuant or Sybr Green I fluorescent nucleic acid stains. Assays with human cell lines are performed in the presence of 0.1 μm PSC833 to inhibit confounding P-gp activity [2].
Animal Research	Oral toxicity of FTC analogs in mice is tested by mixing 50 mg/mL stocks in DMSO 1:1 with Tween 80 (polyoxyethylene sorbitan mono-oleate) and diluting with 5% w/v glucose such that the final volume administered by oral gavage is 10 μL/g of body weight. Pairs of mice are administered oral doses of 50 mg/kg Ko132, Ko134, Ko143, or vehicle under light methoxyflurane anesthesia. Final tests of 50 mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects. Further, another pair of mice receive a higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analog stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5 μL/g of body weight. After pilot tests at lower doses show no adverse effects, mice (4 per group) are administered vehicle or 10 mg/kg i.p. of Ko132, Ko134, or Ko143. The mice are observed continuously during the first hour after administration and then at increasing intervals for 2 weeks, after which they are sacrificed for histological examination of major organs and structures [2].

Chemical Properties

Molecular Weight	469.57
Formula	C₂₆H₃₅N₃O₅
Cas No.	461054-93-3
Smiles	COc1ccc2c3C[C@@H]4N([C@@H](CC(C)C)c3[nH]c2c1)C(=O)[C@H](CCC(=O)OC(C)(C)C)NC4=O
Relative Density.	1.24 g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 90 mg/mL (191.66 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.03 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1296 mL	10.6480 mL	21.2961 mL	106.4804 mL
5 mM	0.4259 mL	2.1296 mL	4.2592 mL	21.2961 mL
10 mM	0.2130 mL	1.0648 mL	2.1296 mL	10.6480 mL
20 mM	0.1065 mL	0.5324 mL	1.0648 mL	5.3240 mL
50 mM	0.0426 mL	0.2130 mL	0.4259 mL	2.1296 mL
100 mM	0.0213 mL	0.1065 mL	0.2130 mL	1.0648 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc