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Chemical Structure| 126411-39-0 Chemical Structure| 126411-39-0

Structure of SR12813
CAS No.: 126411-39-0

Chemical Structure| 126411-39-0

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SR-12813 is a pregnane X receptor (PXR) agonist and HMG-CoA reductase inhibitor with an IC50 of 850 nM.

Synonyms: GW 485801

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Product Details of SR12813

CAS No. :126411-39-0
Formula : C24H42O7P2
M.W : 504.53
SMILES Code : OC1=C(C(C)(C)C)C=C(C=C(P(OCC)(OCC)=O)P(OCC)(OCC)=O)C=C1C(C)(C)C
Synonyms :
GW 485801
MDL No. :MFCD00888473
InChI Key :YQLJDECYQDRSBI-UHFFFAOYSA-N
Pubchem ID :446313

Safety of SR12813

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MCF-7 cells MCF-7 cells Pretreatment led to increased resistance to tamoxifen Cancer Biol Ther. 2009 Jul;8(13):1265-72.
MDA-MB-231 cells MDA-MB-231 cells Pretreatment led to increased resistance to Taxol Cancer Biol Ther. 2009 Jul;8(13):1265-72.
HEK293 cells HEK293 cells To study the effect of SR12813 on PXR mutants, results showed that the C307A mutant restored SR12813-induced DNA binding. JCI Insight. 2024 Jan 23;9(2):e172632.
HepG2 cells HepG2 cells To investigate the effect of SR12813 on PXR transactivation capacity, results showed that GSNO significantly decreased SR12813-induced PXR reporter activity. JCI Insight. 2024 Jan 23;9(2):e172632.
LS174T-hPXR cells LS174T-hPXR cells To investigate the effect of SR12813 on the proliferation of LS174T-hPXR cells. The results showed that SR12813 significantly promoted cell proliferation, which was inhibited by the PXR antagonist SPA70 Cells. 2020 Jul 8;9(7):1641.
22RV1-hPXR cells 22RV1-hPXR cells To investigate the activation of hPXR by SR12813. The results showed that SR12813 significantly activated hPXR, increasing luciferase expression Cells. 2020 Jul 8;9(7):1641.
HepG2-hPXR cells HepG2-hPXR cells To investigate the activation of hPXR by SR12813. The results showed that SR12813 significantly activated hPXR, increasing luciferase expression Cells. 2020 Jul 8;9(7):1641.
LS174T-hPXR cells LS174T-hPXR cells To investigate the activation of hPXR by SR12813. The results showed that SR12813 significantly activated hPXR, increasing luciferase expression Cells. 2020 Jul 8;9(7):1641.
HG5LN GAL4-hPXR cells HG5LN GAL4-hPXR cells To investigate the activation of hPXR by SR12813. The results showed that SR12813 significantly activated hPXR, increasing luciferase expression by about 5-fold Cells. 2020 Jul 8;9(7):1641.
THP-1-Blue NFκB cells THP-1-Blue NFκB cells To evaluate the effect of SR12813 on LPS-induced NFκB signaling, results showed that SR12813 inhibited NFκB signaling. J Pharmacol Exp Ther. 2016 Oct;359(1):91-101.
Caco-2 cells Caco-2 cells To evaluate the protective effect of SR12813 on TNFα/IFNγ-induced intestinal epithelial barrier dysfunction, results showed that SR12813 pretreatment significantly reduced FITC-dextran flux, indicating barrier protection. J Pharmacol Exp Ther. 2016 Oct;359(1):91-101.
hCMEC/D3 cells hCMEC/D3 cells Used as a positive regulator of P-gp to upregulate P-gp abundance Pharm Res. 2024 Jul;41(7):1427-1441.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL

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