Km: 75 μM Estradiol 17-(β-D-Glucuronide) is a substrate of the multidrug resistance protein 2 (MRP2). MRP2 is a member of the superfamily of ATP-binding cassette (ABC) transporters, which transport various molecules across extra- and intra-cellular membranes. MRP2 is a member of the MRP subfamily that is involved in multi-drug resistance. MRP2 is expressed in the apical side of the hepatocyte and functions in biliary transport. In vitro: Estradiol 17-(β-D-Glucuronide) was identified as an ATP dependent, osmotically sensitive transport of the naturally occurring conjugated estrogen, and was found to be readily demonstrable in plasma membrane vesicles from populations of MRP-transfected HeLa cells. The involvement of MRP was confirmed by demonstrating that transport was completely inhibited by a monoclonal antibody specific for an intracellular conformational epitope of the protein . In vivo: Animal study found that estradiol 17-(β-D-Glucuronide) could induce an immediate, profound and reversible inhibition of bile flow after its i.v. administration to the rat. Moreover, the cholestasis degree was found to be dose-dependent in the range of 8.5 to 21 mumol/kg i.v. A dose of 11 mumol/kg i.v. was able to inhibit bile flow and bile acid secretory rate 65 to 70% within 15 to 30 min of its administration. In addition, the bile flow and bile acid secretion returned to near control levels within 3 hours . Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 15087-02-2

Molecular Weight: 470.49

Formula: C24H31NaO8

Chemical Name: sodium (2S,3S,4S,5R,6R)-6-{[(1S,3aS,3bR,9bS,11aS)-7-hydroxy-11a-methyl-1H,2H,3H,3aH,3bH,4H,5H,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl]oxy}-3,4,5-trihydroxyoxane-2-carboxylate

Smiles: [Na+].C[C@]12CC[C@H]3[C@@H](CCC4=CC(O)=CC=C43)[C@@H]1CC[C@@H]2O[C@@H]1O[C@@H]([C@@H](O)[C@H](O)[C@H]1O)C([O-])=O

InChiKey: UQSHTUQZFYMYFO-VGYGJRAWSA-M

InChi: InChI=1S/C24H32O8.Na/c1-24-9-8-14-13-5-3-12(25)10-11(13)2-4-15(14)16(24)6-7-17(24)31-23-20(28)18(26)19(27)21(32-23)22(29)30;/h3,5,10,14-21,23,25-28H,2,4,6-9H2,1H3,(H,29,30);/q;+1/p-1/t14-,15-,16+,17+,18+,19+,20-,21+,23-,24+;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.