All AbMole products are for research use only, cannot be used for human consumption.
Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. Inhibits ABCB1 and ABCC1 at higher concentrations. Rapidly metabolized in rat plasma.
Toxicol Appl Pharmacol. 2024 Sep 24.
Human trophoblast organoids for improved prediction of placental ABC transporter-mediated drug transport
Ko 143 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | MDCK II parent cells and ABCG2-transduced MDCK II cells |
| Preparation method | Reduction of mitoxantrone efflux from ABCG2-transduced MDCK II cells treated with Ko143 (1) or Ko143 analogues 3, 20, 21, and 22 as determined by mitoxantrone fluorescence. Cells were incubated with test compounds and mitoxantrone for 60 min. The mitoxantrone concentration was 1 μM in all experiments. |
| Concentrations | 1 μM |
| Incubation time | 60 min |
| Animal Experiment | |
|---|---|
| Animal models | Female Abcb1a/b(−/−) (Mdr1a/b(−/−) mice |
| Formulation | DMSO concentration of 5% (v/v) with a solution containing 10% (v/v) Tween 80, 25% (v/v) PEG 300, and 65% (v/v) sterile water. |
| Dosages | 1, 7, 15 mg/kg |
| Administration | i.v. injection |
| Molecular Weight | 469.57 |
| Formula | C26H35N3O5 |
| CAS Number | 461054-93-3 |
| Solubility (25°C) | DMSO 23 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BCRP/ABCG2/MXR/ABCP Products |
|---|
| KS176
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter with IC50 values of 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays, respectively. |
| Fumitremorgin C
Fumitremorgin C (FTC) is a fungal toxin of the diketopiperazines family of compounds. |
| YHO-13177
YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2). |
| Zamicastat
Zamicastat is a dopamine β-hydroxylase (DBH) inhibitor that crosses the blood-brain barrier and causes central and peripheral effects. In addition, Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
