An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM)

Estradiol 17-(β-D-Glucuronide) (sodium salt) – 5 mg

Brand:
Cayman
CAS:
15087-02-2
Storage:
-20
UN-No:
Non-Hazardous - /

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.{26342} It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.{26342,26341} In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transport via MRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) (E23G; Item No. 16155).{26341,26340} E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.{26341}  

 

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Description

An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow

Formal name: (17β)-3-hydroxyestra-1,3,5(10)-trien-17-yl β-D-glucopyranosiduronic acid, monosodium salt

Synonyms:  17β-Estradiol 17-(β-D-Glucuronide)|17β-Oestradiol 17-(β-D-Glucuronide)|E217G|β-Estradiol 17-(β-D-Glucuronide)

Molecular weight: 470.5

CAS: 15087-02-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Transporter & Exchanger Modulators||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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