1. Membrane Transporter/Ion Channel
  2. BCRP
  3. Ko 143

Ko 143 

Cat. No.: HY-10010 Purity: 99.79%
Handling Instructions

Ko 143 is a potent and selective ATP-binding cassette sub-family G member 2 (ABCG2) inhibitor.

For research use only. We do not sell to patients.

Ko 143 Chemical Structure

Ko 143 Chemical Structure

CAS No. : 461054-93-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 197 In-stock
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Ko 143 purchased from MCE. Usage Cited in: Drug Deliv. 2017 Nov;24(1):1453-1459.

    Fluorescent substrates accumulate in the organoids. The organoids are incubated in Hoechst 33342 with or without YHO-13177 or Ko143 for 20, 60 and 100 minutes, respectively. Ko143 and YHO-13177 notably decrease the fluorescence intensity of Hoechst 33342 in the organoids.

    Ko 143 purchased from MCE. Usage Cited in: J Drug Target. 2016;24(5):441-9.

    Cells are co-treated with 5 μM of free Raloxifene or an equivalent dose of SMA-raloxifene and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.

    Ko 143 purchased from MCE. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9.

    Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ko 143 is a potent and selective ATP-binding cassette sub-family G member 2 (ABCG2) inhibitor.

    IC50 & Target

    EC90: 26 nM (BCRP)

    In Vitro

    Ko143 (10 nM) significantly decreases (2.5-fold) the IC50 of MTX for HEK G2 cells and mouse G2 cells. Ko143 (1-100 μM) metabolite does not inhibit the function of ABC Transporters[1]. Reversal of drug resistance in topotecan-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by FTC analogue Ko143. Ko143 is applied at zero, one, or eight times the EC90 concentration of 25 nM[2]. Ko143 inhibits BCRP-mediated transport of rosuvastatin 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 topotecan in mice[2]. Ko143 significantly affects the pharmacokinetics of rosuvastatin in rats[3].

    Molecular Weight

    469.57

    Formula

    C₂₆H₃₅N₃O₅

    CAS No.

    461054-93-3

    SMILES

    O=C1N2[[email protected]]([H])(C3=C(C[[email protected]]2(C(N[[email protected]]1CCC(OC(C)(C)C)=O)=O)[H])C4=CC=C(OC)C=C4N3)CC(C)C

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (106.48 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1296 mL 10.6480 mL 21.2961 mL
    5 mM 0.4259 mL 2.1296 mL 4.2592 mL
    10 mM 0.2130 mL 1.0648 mL 2.1296 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.32 mM); Suspended solution; Need ultrasonic and warming and heat to 50°C

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    cells are plated at 400 or 1000/well in 96-well plates the night before addition of drugs. A concentration series of 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Oral toxicity of FTC analogues 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 the higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analogue 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 including brain, salivary glands, heart, lungs, liver, adrenal glands, kidneys, urinary tract, spleen, thymus, bone marrow, pancreas, stomach, intestines, cecum, colon, testes, epididymus, skin, head, trunk, and limbs.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Product Name:
    Ko 143
    Cat. No.:
    HY-10010
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