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SR12813

Catalog No. T6994 CAS 126411-39-0

Synonyms: SR-12813, SR 12813, GW 485801

SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.

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SR12813, CAS 126411-39-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 144.00
50 mg	In stock	$ 243.00
100 mg	In stock	$ 351.00
200 mg	In stock	$ 567.00
1 mL * 10 mM (in DMSO)	In stock	$ 55.00

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Purity: 99.95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.
Targets&IC50	HMG-CoA reductase:850 nM
In vitro	SR12813 is a very potent and efficacious activator of both the human and rabbit PXR, with EC50 values of approximately 200 nM and 700 nM, respectively. By contrast, SR12813 is only a very weak activator of the rat and mouse PXR[1]. SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 μM but has no effect on fatty acid synthesis. SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 μM. The inhibition of HMG-CoA reductase activity is rapid with a T1/2 of 10 min[2].
In vivo	The bisphosphonate ester SR12813 lowers cholesterol levels in a range of species including rats, dogs and primates[1].
Kinase Assay	Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cells are lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassium dihydrophosphate, 30 mM EDTA, 5 mM dithiothreitol, pH 7.4 at room temperature. In some experiments KF is omitted to measure 'total' HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate is further determined.
Cell Research	Hep G2 cells are incubated for 21 h with either 1 μM lovastatin or 3 μM SR-12813 in 5% LPDS medium. mRNA is isolated and analyzed by Northern blotting.(Only for Reference)

Synonyms	SR-12813, SR 12813, GW 485801
Molecular Weight	504.53
Formula	C24H42O7P2
CAS No.	126411-39-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50.5 mg/mL (100 mM)

Ethanol: 50.5 mg/mL (100 mM)

References and Literature

1. Jones SA, et al. Mol Endocrinol. 2000, 14(1):27-39. 2. Berkhout TA, et al. J Biol Chem. 1996, 271(24):14376-82. 3. Berkhout TA, et al. Atherosclerosis. 1997, 133(2):203-12.

Citations

1. Dou X, Huo T, Liu Y, et al.Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.European Journal of Medicinal Chemistry.2024: 116323.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Metabolism Compound Library Anti-Hypertension Compound Library Anti-Cancer Metabolism Compound Library Anti-Metabolism Disease Compound Library Autophagy Compound Library Glutamine Metabolism Compound Library Ferroptosis Compound Library Anti-Cardiovascular Disease Compound Library ReFRAME Related Library

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Rosuvastatin calcium Dalvastatin Atorvastatin lactone 2'-Ethyl Simvastatin Lovastatin HMG499 Cerivastatin sodium Anhydrosimvastatin

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Keywords

SR12813 126411-39-0 Autophagy Metabolism HMG-CoA Reductase GW-485801 SR-12813 HMG-CoA Reductase (HMGCR) inhibit Inhibitor GW485801 SR 12813 GW 485801 inhibitor

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