1. Metabolic Enzyme/Protease
  2. FXR
  3. PX20606

PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy.

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PX20606 Chemical Structure

PX20606 Chemical Structure

CAS No. : 1268245-19-7

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Description

PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
76 nM
Compound: 7
Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
[PMID: 27268696]
Molecular Weight

554.85

Formula

C29H22Cl3NO4

CAS No.
SMILES

O=C(O)C(C=C1)=CC=C1C(C2)C2C3=CC=C(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)C=C3Cl

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Room temperature in continental US; may vary elsewhere.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PX20606
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HY-100443
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