SR 1078 | SR1078 | CAS#1246525-60-9 | f RORα and RORγ agonist

MedKoo Cat#: 526817 | Name: SR-1078

Description:

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

SR-1078 is a selective agonist of RORα and RORγ that stimulates ROR transcriptional activity in HEK293 cell reporter assays at concentrations as low as 2 µM without effect at the related liver X receptors and farnesoid X receptors. SR1078 modulates the conformation of RORγ in a biochemical assay and activates RORα and RORγ driven transcription. SR1078 stimulates expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. SR1078 can be utilized as a chemical tool to probe the function of these receptors both in vitro and in vivo.

Chemical Structure

SR-1078

CAS#1246525-60-9

Theoretical Analysis

MedKoo Cat#: 526817

Name: SR-1078

CAS#: 1246525-60-9

Chemical Formula: C17H10F9NO2

Exact Mass: 431.0568

Molecular Weight: 431.26

Elemental Analysis: C, 47.35; H, 2.34; F, 39.65; N, 3.25; O, 7.42

Price and Availability

Size	Price	Availability
200mg	USD 1,450.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,450.00	2 Weeks

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Synonym

SR-1078; SR 1078; SR1078.

IUPAC/Chemical Name

N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-4-(trifluoromethyl)benzamide

InChi Key

DUXWIYXHHGNUJU-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H10F9NO2/c18-15(19,20)11-3-1-9(2-4-11)13(28)27-12-7-5-10(6-8-12)14(29,16(21,22)23)17(24,25)26/h1-8,29H,(H,27,28)

SMILES Code

O=C(NC1=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C1)C2=CC=C(C(F)(F)F)C=C2

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:

SR-1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.

In vitro activity:

This study describes the identification of SR-1078. SR-1078 modulated the conformation of RORγ in a biochemical assay and activated RORα and RORγ driven transcription. SR-1078 stimulated the expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. Reference: ACS Chem Biol. 2010 Nov 19;5(11):1029-34. https://pubmed.ncbi.nlm.nih.gov/20735016/

In vivo activity:

This study suggests a potential link between RORα, ER stress, and adipose tissue inflammation, offering therapeutic insights for obesity-related diseases. Overexpression of RORα or SR-1078 treatment heightened inflammation and increased macrophage infiltration in obese mice. Additionally, SR-1078 upregulated ER stress response genes and activated UPR signaling pathways. Reference: J Biol Chem. 2017 Aug 25;292(34):13959-13969. https://pubmed.ncbi.nlm.nih.gov/28698385/

	Solvent	mg/mL	mM
Solubility
	DMSO	43.1	100.00
	Ethanol	43.1	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 431.26 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. Wang Y, Solt LA, Kojetin DJ, Burris TP. Regulation of p53 stability and apoptosis by a ROR agonist. PLoS One. 2012;7(4):e34921. doi: 10.1371/journal.pone.0034921. Epub 2012 Apr 11. PMID: 22509368; PMCID: PMC3324542. 2. Wang Y, Kumar N, Nuhant P, Cameron MD, Istrate MA, Roush WR, Griffin PR, Burris TP. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ. ACS Chem Biol. 2010 Nov 19;5(11):1029-34. doi: 10.1021/cb100223d. PMID: 20735016; PMCID: PMC3003750. 3. Liu Y, Chen Y, Zhang J, Liu Y, Zhang Y, Su Z. Retinoic acid receptor-related orphan receptor α stimulates adipose tissue inflammation by modulating endoplasmic reticulum stress. J Biol Chem. 2017 Aug 25;292(34):13959-13969. doi: 10.1074/jbc.M117.782391. Epub 2017 Jul 11. PMID: 28698385; PMCID: PMC5572914. 4. Wang Y, Billon C, Walker JK, Burris TP. Therapeutic Effect of a Synthetic RORα/γ Agonist in an Animal Model of Autism. ACS Chem Neurosci. 2016 Feb 17;7(2):143-8. doi: 10.1021/acschemneuro.5b00159. Epub 2015 Dec 3. PMID: 26625251; PMCID: PMC4759619.

In vitro protocol:

In vivo protocol:

1. Liu Y, Chen Y, Zhang J, Liu Y, Zhang Y, Su Z. Retinoic acid receptor-related orphan receptor α stimulates adipose tissue inflammation by modulating endoplasmic reticulum stress. J Biol Chem. 2017 Aug 25;292(34):13959-13969. doi: 10.1074/jbc.M117.782391. Epub 2017 Jul 11. PMID: 28698385; PMCID: PMC5572914. 2. Wang Y, Billon C, Walker JK, Burris TP. Therapeutic Effect of a Synthetic RORα/γ Agonist in an Animal Model of Autism. ACS Chem Neurosci. 2016 Feb 17;7(2):143-8. doi: 10.1021/acschemneuro.5b00159. Epub 2015 Dec 3. PMID: 26625251; PMCID: PMC4759619.

1: Wang Y, Kumar N, Nuhant P, Cameron MD, Istrate MA, Roush WR, Griffin PR, Burris TP. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ. ACS Chem Biol. 2010 Nov 19;5(11):1029-34. doi: 10.1021/cb100223d. PMID: 20735016; PMCID: PMC3003750. 2: Wang Y, Solt LA, Kojetin DJ, Burris TP. Regulation of p53 stability and apoptosis by a ROR agonist. PLoS One. 2012;7(4):e34921. doi: 10.1371/journal.pone.0034921. Epub 2012 Apr 11. PMID: 22509368; PMCID: PMC3324542. 3: Zhang W, Zhang J, Fang L, Zhou L, Wang S, Xiang Z, Li Y, Wisely B, Zhang G, An G, Wang Y, Leung S, Zhong Z. Increasing human Th17 differentiation through activation of orphan nuclear receptor retinoid acid-related orphan receptor γ (RORγ) by a class of aryl amide compounds. Mol Pharmacol. 2012 Oct;82(4):583-90. doi: 10.1124/mol.112.078667. Epub 2012 Jun 14. PMID: 22700697. 4: Kamata Y, Tominaga M, Sakaguchi A, Umehara Y, Negi O, Ogawa H, Takamori K. Retinoid-related orphan receptor α is involved in induction of semaphorin 3A expression in normal human epidermal keratinocytes. J Dermatol Sci. 2015 Jul;79(1):84-6. doi: 10.1016/j.jdermsci.2015.03.015. Epub 2015 Apr 2. PMID: 25896270. 5: Wang Y, Billon C, Walker JK, Burris TP. Therapeutic Effect of a Synthetic RORα/γ Agonist in an Animal Model of Autism. ACS Chem Neurosci. 2016 Feb 17;7(2):143-8. doi: 10.1021/acschemneuro.5b00159. Epub 2015 Dec 3. PMID: 26625251; PMCID: PMC4759619. 6: Oh TG, Wang SM, Acharya BR, Goode JM, Graham JD, Clarke CL, Yap AS, Muscat GEO. The Nuclear Receptor, RORγ, Regulates Pathways Necessary for Breast Cancer Metastasis. EBioMedicine. 2016 Apr;6:59-72. doi: 10.1016/j.ebiom.2016.02.028. Epub 2016 Feb 18. PMID: 27211549; PMCID: PMC4856749. 7: Zhao Y, Xu L, Ding S, Lin N, Ji Q, Gao L, Su Y, He B, Pu J. Novel protective role of the circadian nuclear receptor retinoic acid-related orphan receptor-α in diabetic cardiomyopathy. J Pineal Res. 2017 Apr;62(3). doi: 10.1111/jpi.12378. Epub 2017 Feb 22. PMID: 27862268. 8: Gascoyne DM, Lyne L, Spearman H, Buffa FM, Soilleux EJ, Banham AH. Vitamin D Receptor Expression in Plasmablastic Lymphoma and Myeloma Cells Confers Susceptibility to Vitamin D. Endocrinology. 2017 Mar 1;158(3):503-515. doi: 10.1210/en.2016-1802. PMID: 28001444; PMCID: PMC5460784. 9: Liu Y, Chen Y, Zhang J, Liu Y, Zhang Y, Su Z. Retinoic acid receptor-related orphan receptor α stimulates adipose tissue inflammation by modulating endoplasmic reticulum stress. J Biol Chem. 2017 Aug 25;292(34):13959-13969. doi: 10.1074/jbc.M117.782391. Epub 2017 Jul 11. PMID: 28698385; PMCID: PMC5572914. 10: Chai C, Cox B, Yaish D, Gross D, Rosenberg N, Amblard F, Shemuelian Z, Gefen M, Korach A, Tirosh O, Lanton T, Link H, Tam J, Permyakova A, Ozhan G, Citrin J, Liao H, Tannous M, Hahn M, Axelrod J, Arretxe E, Alonso C, Martinez-Arranz I, Betés PO, Safadi R, Salhab A, Amer J, Tber Z, Mengshetti S, Giladi H, Schinazi RF, Galun E. Agonist of RORA Attenuates Nonalcoholic Fatty Liver Progression in Mice via Up-regulation of MicroRNA 122. Gastroenterology. 2020 Sep;159(3):999-1014.e9. doi: 10.1053/j.gastro.2020.05.056. Epub 2020 May 22. PMID: 32450149; PMCID: PMC7722250. 11: Lee JE, Choi G, Cho M, Kim D, Lee MO, Chung Y. A critical regulation of Th2 cell responses by RORα in allergic asthma. Sci China Life Sci. 2021 Aug;64(8):1326-1335. doi: 10.1007/s11427-020-1825-3. Epub 2020 Nov 3. PMID: 33165810. 12: Auclair M, Roblot N, Capel E, Fève B, Antoine B. Pharmacological modulation of RORα controls fat browning, adaptive thermogenesis, and body weight in mice. Am J Physiol Endocrinol Metab. 2021 Feb 1;320(2):E219-E233. doi: 10.1152/ajpendo.00131.2020. Epub 2020 Nov 30. PMID: 33252251; PMCID: PMC8260366. 13: Moreno-Smith M, Milazzo G, Tao L, Fekry B, Zhu B, Mohammad MA, Di Giacomo S, Borkar R, Reddy KRK, Capasso M, Vasudevan SA, Sumazin P, Hicks J, Putluri N, Perini G, Eckel-Mahan K, Burris TP, Barbieri E. Restoration of the molecular clock is tumor suppressive in neuroblastoma. Nat Commun. 2021 Jun 28;12(1):4006. doi: 10.1038/s41467-021-24196-4. PMID: 34183658; PMCID: PMC8238982. 14: Liang T, Chen T, Qiu J, Gao W, Qiu X, Zhu Y, Wang X, Chen Y, Zhou H, Deng Z, Li P, Xu C, Peng Y, Liang A, Su P, Gao B, Huang D. Inhibition of nuclear receptor RORα attenuates cartilage damage in osteoarthritis by modulating IL-6/STAT3 pathway. Cell Death Dis. 2021 Sep 28;12(10):886. doi: 10.1038/s41419-021-04170-0. PMID: 34584074; PMCID: PMC8478978. 15: Wang M, Zeng R, Zheng S, Qian Y. Retinoic acid receptor-related orphan receptor alpha and synthetic RORα agonist against invasion and metastasis in tongue squamous cell carcinoma. Biochem Biophys Res Commun. 2024 Nov 12;733:150421. doi: 10.1016/j.bbrc.2024.150421. Epub 2024 Jul 18. PMID: 39047426.