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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
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 bioactive compound 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.
| ln Vitro |
SR1078 is a RORα/RORγ ligand synthesized. In biochemical experiments, SR1078 promotes RORα and RORγ-driven transcription while modifying the structure of RORγ. Additionally, in HepG2 cells expressing both RORα and RORγ, SR1078 also increases the expression of endogenous ROR target genes. SR1078 strongly decreased the constitutive transactivation activity of RORα and RORγ in a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand-binding domain co-transfection test. However, it had no influence on the activities of FXR, LXRα, and LXRβ. In RORα co-transfection tests, treatment of cells with SR1078 (10 μM) led to a considerable increase in transcription. Similarly, SR1078 administration increased RORγ-dependent transcriptional activity in a RORγ co-transfection test [1]. In SH-SY5Y cells, SR1078 (2-10 μM; 24 hours) increased the expression of A2BP1, CYP19A1, NLGN1, and IPTR1 in a dose-dependent manner. The range of EC50 is 3-5 μM [2].
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| ln Vivo |
When SR1078's pharmacokinetic characteristics were investigated in mice, a notable level of exposure was observed. After a single intraperitoneal injection of 10 mg/kg SR1078, the plasma concentration was still over 800 nM 8 hours later, having reached 3.6 μM an hour earlier. These levels were adequate to perform proof-of-principle studies to ascertain whether treatment with SR1078 increases the expression of the ROR target gene in animal models. In order to measure the expression of the G6Pase and FGF21 genes, mice were given SR1078 (10 mg/kg; intraperitoneal); two hours later, the livers were removed and the mRNA was purified. When compared to SR1078 treatment, SR1078 treatment dramatically increased the expression of both FGF21 and G6Pase. control of the vehicle[1]. ?In BTBR mice, SR1078 (10 mg/kg; i.p.) significantly reduced the amount of recurrent grooming behavior by 25% [2].
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| References |
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| Molecular Formula |
C17H10F9NO2
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|---|---|
| Molecular Weight |
431.2576
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| Exact Mass |
431.056
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| CAS # |
1246525-60-9
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| Related CAS # |
1246525-60-9
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| PubChem CID |
17980288
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
362.9±42.0 °C at 760 mmHg
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| Melting Point |
169℃
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| Flash Point |
173.3±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.493
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| LogP |
5.27
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
555
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DUXWIYXHHGNUJU-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-4-(trifluoromethyl)benzamide
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| Synonyms |
SR-1078 SR 1078 SR1078.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~77.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.80 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3188 mL | 11.5939 mL | 23.1879 mL | |
| 5 mM | 0.4638 mL | 2.3188 mL | 4.6376 mL | |
| 10 mM | 0.2319 mL | 1.1594 mL | 2.3188 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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