SR12813 | CAS#126411-39-0 |RXR Agonist

MedKoo Cat#: 532775 | Name: SR12813

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SR12813 is a pan retinoid X receptor (RXR) agonist that is devoid of any RAR activity.

Chemical Structure

SR12813

CAS#126411-39-0

Theoretical Analysis

MedKoo Cat#: 532775

Name: SR12813

CAS#: 126411-39-0

Chemical Formula: C24H42O7P2

Exact Mass: 504.2406

Molecular Weight: 504.54

Elemental Analysis: C, 57.13; H, 8.39; O, 22.20; P, 12.28

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 300.00	2 Weeks
50mg	USD 650.00	2 Weeks

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Related CAS #

No Data

Synonym

SR12813; SR 12813; SR-12813.

IUPAC/Chemical Name

Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate

InChi Key

YQLJDECYQDRSBI-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H42O7P2/c1-11-28-32(26,29-12-2)21(33(27,30-13-3)31-14-4)17-18-15-19(23(5,6)7)22(25)20(16-18)24(8,9)10/h15-17,25H,11-14H2,1-10H3

SMILES Code

O=P(/C(P(OCC)(OCC)=O)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1)(OCC)OCC

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SR12813 is a PXR agonist (EC50 = 200 and 700 nM for human and rabbit PXR, respectively).

In vitro activity:

Dual-targeting of 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMGCR) using statins and SR12813 has potential in anti-cancer treatment. In eight diverse tumor lines, the combination of atorvastatin and SR12813 lowered increased HMGCR expression, and augmented the cytostatic effect of atorvastatin in both statin-resistant and -sensitive cancer cells. Reference: Biochem Biophys Res Commun. 2023 Oct 15;677:13-19. https://pubmed.ncbi.nlm.nih.gov/37541087/

In vivo activity:

The in vivo profile of SR12813 is very similar to direct HMG-CoA reductase inhibitors, although SR12813’s mode of action is unique. SR12813 reduced cholesterol biosynthesis in normolipemic beagle dogs, resulting in a decrease of bile acid excretion, cholesterol excretion and plasma cholesterol level. Reference: Atherosclerosis. 1997 Sep;133(2):203-12. https://pubmed.ncbi.nlm.nih.gov/9298680/

	Solvent	mg/mL	mM
Solubility
	DMSO	50.5	100.00
	Ethanol	50.5	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 504.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhou Y, Tashiro J, Kamatani S, Irie N, Suzuki A, Ishikawa T, Warita K, Oltvai ZN, Warita T. HMG-CoA reductase degrader, SR-12813, counteracts statin-induced upregulation of HMG-CoA reductase and augments the anticancer effect of atorvastatin. Biochem Biophys Res Commun. 2023 Oct 15;677:13-19. doi: 10.1016/j.bbrc.2023.07.056. Epub 2023 Jul 27. PMID: 37541087. 2. Chen Y, Huang W, Chen F, Hu G, Li F, Li J, Xuan A. Pregnane X receptors regulate CYP2C8 and P-glycoprotein to impact on the resistance of NSCLC cells to Taxol. Cancer Med. 2016 Dec;5(12):3564-3571. doi: 10.1002/cam4.960. Epub 2016 Nov 22. PMID: 27878971; PMCID: PMC5224856. 3. Flora GD, Sahli KA, Sasikumar P, Holbrook LM, Stainer AR, AlOuda SK, Crescente M, Sage T, Unsworth AJ, Gibbins JM. Non-genomic effects of the Pregnane X Receptor negatively regulate platelet functions, thrombosis and haemostasis. Sci Rep. 2019 Nov 20;9(1):17210. doi: 10.1038/s41598-019-53218-x. PMID: 31748641; PMCID: PMC6868193. 4. Berkhout TA, Simon HM, Jackson B, Yates J, Pearce N, Groot PH, Bentzen C, Niesor E, Kerns WD, Suckling KE. SR-12813 lowers plasma cholesterol in beagle dogs by decreasing cholesterol biosynthesis. Atherosclerosis. 1997 Sep;133(2):203-12. doi: 10.1016/s0021-9150(97)00131-7. PMID: 9298680.

In vitro protocol:

In vivo protocol:

1. Flora GD, Sahli KA, Sasikumar P, Holbrook LM, Stainer AR, AlOuda SK, Crescente M, Sage T, Unsworth AJ, Gibbins JM. Non-genomic effects of the Pregnane X Receptor negatively regulate platelet functions, thrombosis and haemostasis. Sci Rep. 2019 Nov 20;9(1):17210. doi: 10.1038/s41598-019-53218-x. PMID: 31748641; PMCID: PMC6868193. 2. Berkhout TA, Simon HM, Jackson B, Yates J, Pearce N, Groot PH, Bentzen C, Niesor E, Kerns WD, Suckling KE. SR-12813 lowers plasma cholesterol in beagle dogs by decreasing cholesterol biosynthesis. Atherosclerosis. 1997 Sep;133(2):203-12. doi: 10.1016/s0021-9150(97)00131-7. PMID: 9298680.

1: Lippert WP, Burschka C, Götz K, Kaupp M, Ivanova D, Gaudon C, Sato Y, Antony P, Rochel N, Moras D, Gronemeyer H, Tacke R. Silicon analogues of the RXR-selective retinoid agonist SR11237 (BMS649): chemistry and biology. ChemMedChem. 2009 Jul;4(7):1143-52. doi: 10.1002/cmdc.200900090. PubMed PMID: 19496083. 2: Gendimenico GJ, Stim TB, Corbo M, Janssen B, Mezick JA. A pleiotropic response is induced in F9 embryonal carcinoma cells and rhino mouse skin by All-trans-retinoic acid, a RAR agonist but not by SR11237, a RXR-selective agonist. J Invest Dermatol. 1994 May;102(5):676-80. PubMed PMID: 8176247.