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Chemical Structure| 1246525-60-9 Chemical Structure| 1246525-60-9
Chemical Structure| 1246525-60-9

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CAS No.: 1246525-60-9

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SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). It binds directly to the ligand-binding domain of RORα and RORγ, increasing their transcriptional activity and stimulating RORα/γ target gene transcription.

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Product Details of SR-1078

CAS No. :1246525-60-9
Formula : C17H10F9NO2
M.W : 431.25
SMILES Code : O=C(NC1=CC=C(C(C(F)(F)F)(C(F)(F)F)O)C=C1)C2=CC=C(C(F)(F)F)C=C2
MDL No. :MFCD18782737
InChI Key :DUXWIYXHHGNUJU-UHFFFAOYSA-N
Pubchem ID :17980288

Safety of SR-1078

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
MYCN3 cells 5 μM 24 hours Restoration of BMAL1 mRNA and protein levels PMC8238982
LAN5 cells 10 μM 24 hours Activation of RORα target genes (G6Pase, FGF-21, and BMAL1) transcription PMC8238982
SK-N-AS MYCN-ER cells 5 μM 72 hours Inhibition of MYCN-mediated lipid metabolism PMC8238982
SK-N-BE(2)-C cells 10 μM 24 hours Activation of RORα target genes (G6Pase, FGF-21, and BMAL1) transcription PMC8238982
HEK293 cells 10 μM 24 hours To assess the potential activity of SR1078 on RORβ. Results showed that SR1078 had no activity on RORβ at 10 μM but significantly enhanced the activity of RORα and RORγ. PMC4759619
SH-SY5Y cells 2, 4, 6, 8, 10 μM 24 hours To evaluate the effect of SR1078 on the expression of ASD-associated genes. Results showed that SR1078 dose-dependently increased the expression of A2BP1, CYP19A1, NLGN1, and IPTR1, with EC50s in the range of 3-5 μM. PMC4759619
HepG2 cells 10 μM 24 hours SR1078 treatment resulted in a significant 3-fold increase in FGF21 mRNA expression. G6Pase mRNA expression was also significantly stimulated ~2-fold by SR1078 treatment. PMC3003750
HEK293 cells 10 μM 24 hours SR1078 significantly inhibited the constitutive transactivation activity of ROR α and ROR γ, but had no effect on the activity of FXR, LXR α and LXR β. PMC3003750
Human chondrocytes 1 μM 48 hours SR1078 treatment led to decreased expression of COL2A1 and SOX9, and promoted the expression of MMP13, ADAMTS4, and ADAMTS5 PMC8478978
Huh7 cells 10 μM overnight To test the effect of SR1078 on MIR122 promoter activity, it was found that SR1078 could induce MIR122 promoter activity. PMC7722250

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
BTBR mice Autism model Intraperitoneal injection 10 mg/kg Once daily for two weeks To evaluate the effect of SR1078 on behavior in an autism model. Results showed that SR1078 significantly reduced repetitive grooming behavior in BTBR mice (25% reduction) and increased the expression of ASD-associated genes. PMC4759619
Mice C57BL6 mice Intraperitoneal injection 10 mg/kg Single injection SR1078 treatment significantly stimulated the expression of FGF21 and G6Pase in the liver. PMC3003750
Nude mice LAN5 cell xenograft model Intraperitoneal injection 15 mg/kg Once daily for 14 days Significant inhibition of tumor growth and restoration of BMAL1 protein levels PMC8238982
C57BL/6 mice High-fat diet-induced fatty liver model Intraperitoneal injection 7.5 mg/kg Twice a week for 3 weeks To evaluate the therapeutic effect of RS-2982 on fatty liver, the results showed that RS-2982 significantly reduced hepatic steatosis, inflammation, and fibrosis, and improved insulin resistance and weight gain. PMC7722250

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.19mL

4.64mL

2.32mL
Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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