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Ko143 BCRP inhibitor

Name: Ko143
Brand: Selleck Chemicals
SKU: S7043
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S7043

KO143 is a potent and relatively selective ATP-binding cassette sub-family G member 2 (ABCG2/BCRP) inhibitor. KO143 decreases the ATPase activity of ABCG2 with IC50 of 9.7 nM.

Chemical Structure

Molecular Weight: 469.57

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S704301 DMSO]94 mg/mL]false]Ethanol]94 mg/mL]false]Water]Insoluble]false Purity: 99.94%

99.94

Related Targets	CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel MCT Amino acid transporter GLUT CRM1 VDAC NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
Related Products	CP-100356 hydrochloride ABCG2 Antibody [H14N12] KS176 YHO-13177 BCRP/ABCG2 Antibody [C19D24]

Chemical Information, Storage & Stability

Molecular Weight	469.57	Formula	C₂₆H₃₅N₃O₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	461054-93-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)CC1C2=C(CC3N1C(=O)C(NC3=O)CCC(=O)OC(C)(C)C)C4=C(N2)C=C(C=C4)OC

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (200.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.350mg/ml (5.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 47 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.780mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	BCRP ^[1] (Cell-free assay) 9.7 nM
In vitro	Ko143, a nontoxic analog of fungal toxin fumitremorgin C, is a potent inhibitor of ABCG2. This compound has an effect on the transport activity of both ABCB1 and ABCC1. Furthermore, it is found to be unstable in rat plasma. These findings indicate that this chemical lacks specificity for ABCG2.^[1]
In vivo	[¹¹C]Ko143 is extensively metabolized in vivo and unidentified radiolabeled metabolites are found in all investigated tissues. This compound and possibly its radiolabeled metabolites are transported by Abcb1a and not by Abcg2 at the mouse blood-brain barrier. [¹¹C]Ko143-derived radioactivity undergoes both hepatobiliary and urinary excretion, with Abcg2 playing a possible role in mediating the transport of radiolabeled metabolites of this chemical from the kidney into urine.^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/26148857/ [2] https://pubmed.ncbi.nlm.nih.gov/29360507/

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