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Merck

K2144

Sigma-Aldrich

Ko143 hydrate

≥98% (HPLC), powder, BCRP inhibitor

Szinonimák:

(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-( 2-methylpropyl)-1,4-dioxopyrazino[1′,2′:1,6]pyrido[3,4- b]indole-3-propanoic acid 1,1-dimethylethyl ester hydrate, Ko-143 hydrate

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez

Méret kiválasztása

1 MG
52 300,00 Ft
5 MG
197 000,00 Ft

52 300,00 Ft


Az elérhetőséggel kapcsolatos kérdésekkel kérjük, forduljon Vevőszolgálatunkhoz.

Megrendelés igénylése nagy tételben

Méret kiválasztása

Nézet módosítása
1 MG
52 300,00 Ft
5 MG
197 000,00 Ft

About This Item

Tapasztalati képlet (Hill-képlet):
C26H35N3O5 · xH2O
CAS-szám:
Molekulatömeg:
469.57 (anhydrous basis)
MDL-szám:
UNSPSC kód:
12352200
PubChem Substance ID:
NACRES:
NA.77

52 300,00 Ft


Az elérhetőséggel kapcsolatos kérdésekkel kérjük, forduljon Vevőszolgálatunkhoz.

Megrendelés igénylése nagy tételben

Terméknév

Ko143 hydrate, ≥98% (HPLC)

Minőségi szint

Teszt

≥98% (HPLC)

Forma

powder

szín

white to off-white

oldhatóság

DMSO: >10 mg/mL

kezdeményező

GlaxoSmithKline

tárolási hőmérséklet

room temp

SMILES string

O.COc1ccc2c3C[C@@H]4N([C@@H](CC(C)C)c3[nH]c2c1)C(=O)[C@H](CCC(=O)OC(C)(C)C)NC4=O

InChI

1S/C26H35N3O5.H2O/c1-14(2)11-20-23-17(16-8-7-15(33-6)12-19(16)27-23)13-21-24(31)28-18(25(32)29(20)21)9-10-22(30)34-26(3,4)5;/h7-8,12,14,18,20-21,27H,9-11,13H2,1-6H3,(H,28,31);1H2/t18-,20-,21-;/m0./s1

Nemzetközi kémiai azonosító kulcs

ZXXZDXPNJJZRDC-PSLBYKFTSA-N

Alkalmazás

Ko143 hydrate has been used:
  • to determine the role of ATP-binding cassette sub-family G member 2 (ABCG2), human embryonic kidney (HEK)-C1 and HEK-ABCG2 in tumor microenvironment[1]
  • to inhibit ABCG2 for sphere formation assay[2]
  • in calcein-AM efflux inhibition to monitor multidrug resistance protein (MRP)-function in kidney[3]
  • for cell viability assay[4]

Biokémiai/fiziológiai hatások

Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone.
Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone. The ABCG2 transporter breast cancer resistance protein (BCRP) plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. It increases intracellular drug accumulation and reverse BCRP-mediated multidrug resistance. It blocked topotecan and ABZSO transport in a concentration-dependent manner. Ko143 is reported to be a more specific inhibitor of BCRP than other known inhibitors of BCRP such as fumitremorgin C and GF120918.
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone.
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner.

Tulajdonságok és előnyök

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Tárolás és stabilitás

The stability of this product in solution has not been determined. According to various sources this product can be stored in solvent (DMSO) at -80°C for 6 months and -20°C for 1 month.

Piktogramok

Exclamation mark

Figyelmeztetés

Warning

Figyelmeztető mondatok

Veszélyességi osztályok

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Célzott szervek

Respiratory system

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable


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Analitikai tanúsítványok (COA)

Lot/Batch Number

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Dokumentumtár megtekintése

Az ügyfelek ezeket is megtekintették

Architecture of chimeric spheroids controls drug transport
Curran S, et al.
Cancer Microenvironment, 8(2), 101-109 (2015)
Multi-drug resistance ABC transporter inhibition enhances murine ventral prostate stem/progenitor cell differentiation
Samant MD, et al.
Stem Cells and Development, 24(10), 1236-1251 (2015)
Jae Guen Song et al.
Cancer chemotherapy and pharmacology, 78(4), 735-744 (2016-08-16)
The present study aimed to discover a new potent BCRP inhibitor overcoming multidrug resistance. Effects of LW6 on the functional activity and gene expression of two major efflux transporters, BCRP and P-gp, were evaluated by using MDCKII cells overexpressing each
Cong Duan et al.
Biopharmaceutics & drug disposition, 38(1), 75-83 (2016-12-08)
Lindera aggregata (Sims) Kosterm root has been used in traditional Chinese medicine for the treatment of rheumatism palsy, dyspepsia and frequent urination for a long time. Norisoboldine, the main active constituent of this herb drug, possesses outstanding anti-arthritis activity. However
Lu Xiao et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 93, 456-467 (2016-09-03)
Efflux transporters are extensively distributed and expressed in the intestinal epithelium and contribute to the low oral bioavailability of flavonoids and flavonoid glucuronides by pumping these compounds back into intestinal lumen. Our previous study has shown the inhibitory effect of

Cikkek

Protein-based drug transporters are expressed in Sf9 cells. Understanding the specific mechanisms of tumor cell transporters is an essential aspect of chemotherapeutic drug design.

Discover Bioactive Small Molecules for ADME/Tox

Questions

  1. Dear all, once I dissolved  the compound in DMSO I should store it in the fridge or at lower temperatures? 

    1 answer
    1. The stability of this product in solution has not been determined. According to various sources this product can be stored in solvent (DMSO) at -80°C for 6 months and -20°C for 1 month. This information has not been validated.

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