1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  2. LXR FXR ROR Apoptosis
  3. T0901317

T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

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T0901317 Chemical Structure

T0901317 Chemical Structure

CAS No. : 293754-55-9

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10 mM * 1 mL in DMSO
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Based on 20 publication(s) in Google Scholar

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Description

T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα[1]. T0901317 activates FXR with an EC50 of 5 μM[2]. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice[4][5].

IC50 & Target

EC50: 20 nM (LXRα) and 5 μM (FXR)[1][2]
Ki: 132 nM (RORα) and 51 nM (RORγ)[3]

In Vitro

rateand the T0901317 (5-50 μM; 72 hours) significantly inhibits cellular proliferation in CaOV3, SKOV3, A2780 (human ovarian carcinoma cell lines) in a dose-dependent and time-dependent manner[5].
T0901317 (10 μM; 24-72 hours) decreases the percentage of cells in S phase and increases the percentage of cells in the G0/G1 phase, indicating a cell cycle arrest at the G1-S checkpoint. The percentage of cells in G0/G1 phase increases in a time-dependent manner[5].
T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis[5].
T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[5]

Cell Line: A2780, CaOV3 and SKOV3 ovarian cancer cell lines
Concentration: 5, 10, 20, 40 or 50 μM
Incubation Time: 72 hours
Result: Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner.

Cell Cycle Analysis[5]

Cell Line: A2780, CaOV3 and SKOV3 cells
Concentration: 10 μM
Incubation Time: 24, 48 or 72 hours
Result: Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase.

Apoptosis Analysis[5]

Cell Line: CaOV3 cells
Concentration: 10 to 40 μM
Incubation Time: 24 hours
Result: Resulted in a significant increase of cells in early apoptosis.

Western Blot Analysis[5]

Cell Line: CaOV3 cells
Concentration: 5 to 40 μM
Incubation Time: 48 hours
Result: Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.
In Vivo

T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis[5].
T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8- to 10-week-old LDL receptor null mice[5]
Dosage: 10 mg/kg
Administration: Orally; daily; for 12 weeks
Result: Inhibited the progression of atherosclerosis.
Molecular Weight

481.33

Formula

C17H12F9NO3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(N(CC(F)(F)F)S(C2=CC=CC=C2)(=O)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (207.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (207.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0776 mL 10.3879 mL 20.7758 mL
5 mM 0.4155 mL 2.0776 mL 4.1552 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.0776 mL 10.3879 mL 20.7758 mL 51.9394 mL
5 mM 0.4155 mL 2.0776 mL 4.1552 mL 10.3879 mL
10 mM 0.2078 mL 1.0388 mL 2.0776 mL 5.1939 mL
15 mM 0.1385 mL 0.6925 mL 1.3851 mL 3.4626 mL
20 mM 0.1039 mL 0.5194 mL 1.0388 mL 2.5970 mL
25 mM 0.0831 mL 0.4155 mL 0.8310 mL 2.0776 mL
30 mM 0.0693 mL 0.3463 mL 0.6925 mL 1.7313 mL
40 mM 0.0519 mL 0.2597 mL 0.5194 mL 1.2985 mL
50 mM 0.0416 mL 0.2078 mL 0.4155 mL 1.0388 mL
60 mM 0.0346 mL 0.1731 mL 0.3463 mL 0.8657 mL
80 mM 0.0260 mL 0.1298 mL 0.2597 mL 0.6492 mL
100 mM 0.0208 mL 0.1039 mL 0.2078 mL 0.5194 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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T0901317
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