SR1078
Catalog No.: GC16392Purity:>99.50%Synonyms: SR 1078;SR-1078
SR1078 is an agonist of the retinoic acid receptor-related orphan receptors (RORs) RORα and RORγ, with IC50 values of 1-3µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1246525-60-9
1mgIn Stock
$30.00
1
5mgIn Stock
$70.00
1
10mgIn Stock
$90.00
1
50mgIn Stock
$336.00
1
200mgIn Stock
$1,153.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 1mg | $30.00 | In Stock | 1 | |
| 5mg | $70.00 | In Stock | 1 | |
| 10mg | $90.00 | In Stock | 1 | |
| 50mg | $336.00 | In Stock | 1 | |
| 200mg | $1,153.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
SR1078 is an agonist of the retinoic acid receptor-related orphan receptors (RORs) RORα and RORγ, with IC50 values of 1-3µM[1]. SR1078 can directly bind to the ligand binding domains of RORα and RORγ, increasing the transcriptional activity of these receptors, thereby stimulating the transcription of RORα/γ target genes[2, 3]. SR1078 can regulate osteoblast metabolism through anti-inflammatory effects[4].
In vitro, SR1078 (2-10µM) treatment of human neuroblastoma SH-SY5Y cells for 24h increased the expression of A2BP1, CYP19A1, NLGN1 and IPTR1 genes in the cells in a dose-dependent manner, with an EC50 range of 3-5μM[5]. SR1078 (1, 5µM) treatment of HepG2 cells increased the expression of p53 protein and induced cell apoptosis[6].
In vivo, SR1078 (20mg/kg) was intraperitoneally injected into mice bearing colorectal cancer cell xenografts, significantly inhibiting the growth of subcutaneous tumors and the metastasis of tumor cells[7].
References:
[1] Wang Y, Kumar N, Nuhant P, et al. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ[J]. ACS chemical biology, 2010, 5(11): 1029-1034.
[2] Kamenecka T M, Lyda B, Chang M R, et al. Synthetic modulators of the retinoic acid receptor-related orphan receptors[J]. MedChemComm, 2013, 4(5): 764-776.
[3] Nematisouldaragh D, Kirshenbaum E, Uzonna M, et al. The Role of Retinoic-Acid-Related Orphan Receptor (RORs) in Cellular Homeostasis[J]. International Journal of Molecular Sciences, 2024, 25(21): 11340.
[4] Fernandes J, Benderdor M, Shi Q. SR1078, A synthetic ligand of nuclear receptor ror alpha, modulates osteoblast metabolism with anti-inflammatory effects[J]. Osteoarthritis and Cartilage, 2012, 20: S115-S116.
[5] Wang Y, Billon C, Walker J K, et al. Therapeutic effect of a synthetic RORα/γ agonist in an animal model of autism[J]. ACS Chemical Neuroscience, 2016, 7(2): 143-148.
[6] Wang Y, Solt L A, Kojetin D J, et al. Regulation of p53 stability and apoptosis by a ROR agonist[J]. PloS one, 2012, 7(4): e34921.
[7] Wang Y N, Ruan D Y, Wang Z X, et al. Targeting the cholesterol-RORα/γ axis inhibits colorectal cancer progression through degrading c-myc[J]. Oncogene, 2022, 41(49): 5266-5278.
Protocol
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells |
Preparation Method | SH-SY5Y were treated with SR1078 (2-10µM), and after 24h cells were harvested and cDNA prepared to assess the expression of autism spectrum disorder (ASD)-associated genes by quantitative PCR. |
Reaction Conditions | 2-10µM; 24h |
Applications | SR1078 increases the expression of ASD-associated genes in SH-SY5Y cells. SR1078 treatment increased the expression of A2BP1, CYP19A1, NLGN1, and IPTR1 in a dose-dependent manner with EC50 ranging from 3-5μM. |
| Animal experiment [2]: | |
Animal models | Female BALB/c athymic nude mice |
Preparation Method | To establish the subcutaneous tumour model, 2×106 CRC cells were suspended in 100μL PBS and then injected subcutaneously. Tumour volumes were measured every 3 or 4 days with a caliper and were calculated. For the drug treatment studies, daily doses of 20mg/kg atorvastatin, 20mg/kg SR1078 or the combination were administered via intraperitoneal (i.p.) injection. After the mice were euthanized, the tumours were excised and weighed. |
Dosage form | 20mg/kg; i.p. |
Applications | SR1078 significantly inhibited tumour growth in nude mice subcutaneously. |
References: | |
Product Documents
Purity:>99.50%Appearance:A solid
Chemical Properties
CAS No.
1246525-60-9
Synonyms
SR 1078;SR-1078
Chemical Name
N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-(trifluoromethyl)benzamide
SMILES
C1=CC(=CC=C1C(=O)NC2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O)C(F)(F)F
Molecular Formula
C17H10F9NO2
Molecular Weight
431.25
Solubility
≥ 43.2 mg/mL in DMSO, ≥ 43.4 mg/mL in EtOH
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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