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Chemical Structure| 293754-55-9 Chemical Structure| 293754-55-9

Structure of T0901317
CAS No.: 293754-55-9

Chemical Structure| 293754-55-9

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T0901317 is a selective agonist for LXR and FXR with EC50 of 50 nM and 5 μM, respectively.

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Product Details of T0901317

CAS No. :293754-55-9
Formula : C17H12F9NO3S
M.W : 481.33
SMILES Code : O=S(C1=CC=CC=C1)(N(CC(F)(F)F)C2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)=O
MDL No. :MFCD03412028
InChI Key :SGIWFELWJPNFDH-UHFFFAOYSA-N
Pubchem ID :447912

Safety of T0901317

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 0.1 - 0.5 μM 18 h T317 dose-dependently increased REPS2 expression and inhibited the proliferation and migration of HCC cells. PMC9958117
BNLCL.2 0.1 - 0.5 μM 18 h T317 significantly induced REPS2 protein expression in BNLCL.2 cells. PMC9958117
Huh-7 0.1 - 0.5 μM 18 h T317 significantly induced REPS2 protein expression in Huh-7 cells. PMC9958117
LO2 0.1 - 0.5 μM 18 h T317 significantly induced REPS2 protein expression in LO2 cells. PMC9958117
U2OS cells 10 μM 2 days Inhibited cell proliferation, reduced KI-67 and PCNA protein levels PMC9867777
HOS-MNNG cells 10 μM 2 days Inhibited cell proliferation, reduced KI-67 and PCNA protein levels PMC9867777
Saos-2 cells 10 μM 2 days Inhibited cell proliferation, reduced KI-67 and PCNA protein levels PMC9867777
HEK293 cells 20 nM 20 hours T0901317 induced transcriptional activity of LXR /H9251 with an EC50 of 20 nM, showing higher activity than the endogenous ligand 24,25-EC. PMC317060
primary human monocyte-derived macrophages 1 µM 3 hours T0901317 enhanced the expression of LXR-dependent genes including ABCA1, ABCG1, SMPDL3A, and MERTK. PMC8027700
CD4SP thymocytes 5 μM/ml 4 hours To investigate whether LXRβ directly binds to the 5′-regulatory region of the Il7r gene and promotes its transcription PMC8322414
HL-1 cardiomyocytes 10 μM 6 hours To evaluate the protective effects of T0901317 on LPS-stimulated HL-1 cardiomyocytes, the results showed that T0901317 reversed abnormal cholesterol metabolism, NLRP3 pathway, and inflammatory response. PMC10189481
HCC cells 5 µM 72 hours T0901317 induced fatty acid synthase (FASN) expression in all HCC cells and antagonized TGF β-induced fibrotic marker responses in a subset of HCC cells. PMC6522550
CAFs 5 µM 74 hours T0901317 induced FASN expression in CAFs and suppressed TGF β-induced myofibroblast gene expression. PMC6522550
Hepatocytes 10 μM GF2 significantly reduced T0901317-induced fat accumulation to a similar degree as the control group PMC10785242
Macrophages 10 μM GF2 reduced the expression of pro-inflammatory cytokine genes but did not affect Abca1 expression PMC10785242

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice LXRβ-deficient mice Intraperitoneal injection 0.2 mg/d per mouse 7 continuous days To investigate the effect of T0901317 on the survival of SP thymocytes in LXRβ-deficient mice, the results showed that T0901317 promoted the survival of SP thymocytes in the presence of LXRβ, but had no significant effect in LXRβ-deficient mice PMC8322414
BALB/c Nude mice Subcutaneous tumour model Subcutaneous injection 1 μg Every 3 days, until the end of the experiment Inhibited tumour growth, significantly reduced tumour volume and weight PMC9867777
Mice and hamsters C57BL/6 mice and Golden Syrian hamsters Oral 5 mg/kg Once daily for 7 days T0901317 significantly increased plasma triglyceride and phospholipid levels in mice and hamsters by activating LXR, and induced the expression of genes associated with fatty acid biosynthesis. PMC317060
C57BL/6 or Balbc mice Cecal ligation and puncture (CLP) model Intraperitoneal injection 10 mg/kg Single administration To evaluate the protective effects of T0901317 on CLP model mice, the results showed that T0901317 significantly reduced sepsis score and improved cardiac dysfunction. PMC10189481
Mice High-fat diet-induced MASLD model Oral 50 mg/kg Once daily for 6 weeks GF2 ameliorated high-fat diet-induced MASLD, reducing hepatic fat accumulation and inflammatory response PMC10785242
C57BL/6 mice Wild-type mice Intraperitoneal injection 5 mg/kg Once daily for 10 days T317 significantly increased REPS2 protein and mRNA levels in the liver of mice. PMC9958117

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.39mL

2.08mL

1.04mL

20.78mL

4.16mL

2.08mL

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

References

 

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