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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.
K2144
Ko143 hydrate
≥98% (HPLC), powder, BCRP inhibitor
Synonyme(s) :
(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
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1 MG
171.00 CHF
5 MG
475.00 CHF
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Changer de vue
1 MG
171.00 CHF
5 MG
475.00 CHF
About This Item
Formule empirique (notation de Hill):
C26H35N3O5 · xH2O
Numéro CAS:
Poids moléculaire :
469.57 (anhydrous basis)
Numéro MDL:
Code UNSPSC :
12352200
ID de substance PubChem :
Nomenclature NACRES :
NA.77
Produits recommandés
Nom du produit
Ko143 hydrate, ≥98% (HPLC)
Niveau de qualité
Essai
≥98% (HPLC)
Forme
powder
Couleur
white to off-white
Solubilité
DMSO: >10 mg/mL
Auteur
GlaxoSmithKline
Température de stockage
room temp
Chaîne SMILES
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
Clé InChI
ZXXZDXPNJJZRDC-PSLBYKFTSA-N
Application
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]
Actions biochimiques/physiologiques
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.
Caractéristiques et avantages
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.
Stockage et stabilité
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.
Mention d'avertissement
Warning
Mentions de danger
Conseils de prudence
Classification des risques
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
Organes cibles
Respiratory system
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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Les clients ont également consulté
Makiko Nakamura et al.
Drug metabolism and pharmacokinetics, 33(1), 77-81 (2018-01-18)
Hyperuricemia induces gout and kidney stones and accelerates the progression of renal and cardiovascular diseases. Adenosine 5'-triphosphate-binding cassette subfamily G member 2 (ABCG2) is a urate transporter, and common dysfunctional variants of ABCG2, non-functional Q126X (rs72552713) and semi-functional Q141K (rs2231142)
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)
Architecture of chimeric spheroids controls drug transport
Curran S, et al.
Cancer Microenvironment, 8(2), 101-109 (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
Articles
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.
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Dear all, once I dissolved the compound in DMSO I should store it in the fridge or at lower temperatures?
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