T0901317

For research use only.

Catalog No.S7076

7 publications

T0901317 Chemical Structure

Molecular Weight(MW): 481.33

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

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Selleck's T0901317 has been cited by 7 publications

3 Customer Reviews

  • (C) Cells were pretreated with DMSO or T0901317 (5 μM), then incubated with 100 mg/L ox-LDL for 6 h.

    FEBS Lett, 2015, 589(1):52-8. . T0901317 purchased from Selleck.

    THP-1 macrophages were pretreated with 5 μg/mL T0901317 for 30 min and incubated with 100 μmol/L Hcy for 24 h. protein levels were determined.

    Life Sci, 2018, doi:10.1016/j.lfs.2018.10.060. T0901317 purchased from Selleck.

  • a Entrapment and loading efficiencies of T0901317- liposomes and anti-ICAM-1-T0901317- liposomes at two lipid to T0901317 weight ratios (5:1 and 10:1). b In vitro drug release of T0901317- liposomes (squares) and anti-ICAM-1-T0901317- liposomes (circles) at different time points. Values are expressed as the means ± SD (n = 3)

    Nanoscale Res Lett, 2017, 12(1):322. T0901317 purchased from Selleck.

Purity & Quality Control

Choose Selective Liver X Receptor Inhibitors

Biological Activity

Description T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.
Targets
LXR [1]
(Cell reporter assay)
FXR [2]
50 nM(EC50) 5 μM(EC50)
In vitro

T0901317 acts through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. T0901317 upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism.[1] T0901317 displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs), 10-fold more potent than natural FXR ligand chenodeoxycholic acid. [2] T0901317, is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. [3] T0901317 decreases amyloid-β production in primary neurons in vitro. [4] T0901317 is found to directly bind to RORα and RORγ with high affinity (Ki = 132 and 51 nM, respectively), resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 represses RORα/γ-dependent transactivation of ROR-responsive reporter genes and in HepG2 cells reduces recruitment of steroid receptor coactivator-2 by RORα at an endogenous ROR target gene (G6Pase). [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells MlPtSpVv[3Srb36gZZN{[Xl? NV\wTooxW3SrbYXsZZRqd25ib3[gX|NJZWOqb3zld5Rmem:uIHXm[ox2gCCrbjDoeY1idiCWSGCxJIZw[W1iY3XscJMhdG:jZHXkJJdqfGhiYXOtUGRNNCCHQ{WwQVMhdk1? NWW3WmYxOTl7NkK4PVI>
COS7 cells NGLnfYVHfW6ldHnvckBie3OjeR?= MVixOkBp M3TCTmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDy[YNmeHSxcjD0doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTB;MUGgcm0> NV64fpE1OTd3OEe1O|M>
CHO cells MoTPSpVv[3Srb36gZZN{[Xl? NX3sWnIzSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFJiYnX0ZUBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHL5JJJmeG:{dHXyJIF{e2G7LDDFR|UxRTF4IH7N MnTnNVk5PTN2NkK=
HEK293 cells MnruSpVv[3Srb36gZZN{[Xl? M1LUe2Fod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgS4FtPCC2cnHud4FkfGm4YYTpc44tKEWFNUC9NVkhdk1? NGD5N2gzODN3MECwOS=>
mouse J774 cells NHS3cHBHfW6ldHnvckBie3OjeR?= MmPJRYdwdmm|dDDhZ5Rqfmm2eTDheEBNYFKkZYThJIlvKG2xdYPlJGo4PzRiY3XscJMh[XO|ZYPz[YQh[XNidYDy[Yd2dGG2aX;uJI9nKEGEQ1GxJI1TVkFiZYjwdoV{e2mxbjygSWM2OD1yLkCyO{DPxE1? NHnvc20yQTh3M{S2Ni=>
mouse J774A1 cells M{nkPWZ2dmO2aX;uJIF{e2G7 NHrkdHEyQCCq Mo\YTY5lfWO2aX;uJI9nKEGEQ1GxJI1TVkFiZYjwdoV{e2mxbjDpckBud3W|ZTDKO|c1STFiY3XscJMh[W[2ZYKgNVghcHK|IHL5JHJVNVCFUjygSWM2OD1yLECzOEDPxE1? NELOfYEyQTN7NEizNi=>
HuH7 cells MYjGeY5kfGmxbjDhd5NigQ>? NV;pXHA3XXC{ZXf1cIF1cW:wIH;mJHNTTUJzYzDtVm5CKGyndnXsJIlvKGi3bXHuJGh2UDdiY3XscJMtKEWFNUC9NE4xOzZizszN NUPUXGpkOjB|OEKwNVk>
HepG2 cells NUTLUm1wTnWwY4Tpc44h[XO|YYm= MmXSSYZn\WO2IH;uJHNTTUKSMXOg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzMEBGSzVyPUCuNFYyKM7:TR?= Ml\GNVg6PzN{OEi=
SH-SY5Y cells MWrGeY5kfGmxbjDhd5NigQ>? MoXLNlQhcA>? MlrvRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHJj\XSjIHX4dJJme3OnZDDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOE1NSkRiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkC3OUDPxE1? MXexPVI3PDR6MR?=
CV1 cells NVH0WZcxTnWwY4Tpc44h[XO|YYm= M3;0[nRz[W6|YXP0bZZifGmxbjDv[kBNYFKkZYThJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEOYMTDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE4yPCEQvF2= MUWyOVQ{PTF3MR?=
human H4 cells Mke0SpVv[3Srb36gZZN{[Xl? M2jnS2Vn\mWldDDvckBo[W2vYT3z[YNz\XSjc3WgZYN1cX[rdImgbY4hcHWvYX6gTFQh[2WubIOg[ZhxemW|c3nu[{BCWFB4OUWgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iQX35cI9q\CCkZYThMVQzKG[xcn3heIlwdiCOUFXDUEBie3OjeTygSWM2OD1|Lk[g{txO NXTZbo1ROTd5MkOyPVg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
LXR-β / LXR-α ; 

PubMed: 28097086     


LXRa and LXRb protein expressions were assayed using western blot analysis.

EGFR / p-PI3K p55 / p-PI3K p85 / PI3K p85 / p-PDK1 / PDK1 ; 

PubMed: 28097086     


Western blot analysis was performed using the indicated antibodies after A549 cells were treated with 5 lM T0901317 for different days.

28097086
In vivo T0901317 treatment of 11-week-old APP23 mice for 6 days shows a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)β- to sAPPα-cleavage products. Most importantly, the treatment causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice. [4]

Protocol

Animal Research:

[4]

- Collapse
  • Animal Models: APP23 mice
  • Dosages: 50 mg/kg/day
  • Administration: gastric gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.44 mM)
Ethanol 96 mg/mL (199.44 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+35% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
6mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 481.33
Formula

C17H12F9NO3S

CAS No. 293754-55-9
Storage powder
in solvent
Synonyms N/A
Smiles OC(C1=CC=C(C=C1)N(CC(F)(F)F)[S](=O)(=O)C2=CC=CC=C2)(C(F)(F)F)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID