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  3. Raloxifene 6-glucuronide

Raloxifene 6-glucuronide 

Cat. No.: HY-135581
Handling Instructions

Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.

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Raloxifene 6-glucuronide Chemical Structure

Raloxifene 6-glucuronide Chemical Structure

CAS No. : 174264-50-7

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Description

Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].

IC50 & Target

IC50: 290 μM (Estrogen receptor)[2]

In Vitro

Expressed UGT1A8 catalyzes Raloxifene 6-glucuronide with an apparent Km of 7.9 μM and a Vmax of 0.61 nmol/min/mg of protein. Based on rates of Raloxifene glucuronidation and known extrahepatic expression, UGT1A8 and 1A10 appear to be primary contributors to Raloxifene glucuronidation in human jejunum microsomes. For human liver microsomes, the variability of Raloxifene 6-glucuronide formation is 3-fold. Correlation analyses reveals that UGT1A1 is responsible for Raloxifene 6-glucuronide but not Raloxifene 4'-glucuronide in liver. Treatment of expressed UGTs with alamethicin results in minor increases in enzyme activity, whereas in human intestinal microsomes, maximal increases of 8-fold for the Raloxifene 6-glucuronide are observed. Intrinsic clearance values in intestinal microsomes are 17 μl/min/mg for the Raloxifene 6-glucuronide[2].

Molecular Weight

649.71

Formula

C₃₄H₃₅NO₁₀S

CAS No.

174264-50-7

SMILES

O[[email protected]]([[email protected]]([[email protected]@H]([[email protected]@H](C(O)=O)O1)O)O)[[email protected]@H]1OC2=CC=C(C(C(C3=CC=C(OCCN4CCCCC4)C=C3)=O)=C(C5=CC=C(O)C=C5)S6)C6=C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Raloxifene 6-glucuronideEstrogen Receptor/ERRRaloxifenemetaboliteTGFβ3UGT1A1UGT1A8vitellogeninUGTInhibitorinhibitorinhibit

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Raloxifene 6-glucuronide
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HY-135581
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