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PX20350

PX20350 is a FXR agonist with EC₅₀s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models.

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CAS. Nr.: 1198085-23-2
Formel: C₂₈H₂₂Cl₂F₃N₃O₄
Molecular Weight:592.39

Speicherung:

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

Data Sheet (269 KB)

PX20350 Chemical Structure

CAS. Nr.: 1198085-23-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at androgen receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at androgen receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at CAR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at CAR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at ERalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at ERalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at ERbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at ERbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at GR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at GR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at LXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at LXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at LXRbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at LXRbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at mineralocorticoid receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at mineralocorticoid receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at PPARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at PPARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at PPAR-beta/delta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at PPAR-beta/delta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at PPARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at PPARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at progesterone receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at progesterone receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at RARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at RARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at RARbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at RARbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at RARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at RARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at RXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at RXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at TRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at TRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	>10 μM Compound: 22	Agonist activity at VDR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at VDR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	30 nM Compound: 22	Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	3871 μM Compound: 22	Agonist activity at PXR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay Agonist activity at PXR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay	[PMID: 20638278]
HEK293	EC₅₀	6 nM Compound: 22	Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay	[PMID: 20638278]

Chemical Information

CAS. Nr. 1198085-23-2
Molecular Weight 592.39
Formel C₂₈H₂₂Cl₂F₃N₃O₄
SMILES

O=C(C1=CC=C(CN(C)C2=CC=C(OCC3=C(C4CC4)ON=C3C5=C(Cl)C=CC=C5Cl)N=C2C(F)(F)F)C=C1)O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Deuschle U, et al. FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model. PLoS One. 2012;7(10):e43044. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
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Chemical Information
Reinheit & Dokumentation
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