Turofexorate Isopropyl (XL335)

Catalog No.S2694 Synonyms: Fxr 450

Turofexorate Isopropyl (XL335) Chemical Structure

Molecular Weight(MW): 438.47

Turofexorate Isopropyl (XL335) is a potent, selective FXR agonist with EC50 of 4 nM, highly selective versus other nuclear receptors, such as LXR, PPAR, ER and etc. Phase 1.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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  • Oncotarget, 2015, 6(6):4226-38.. Turofexorate Isopropyl (XL335) purchased from Selleck.

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Notes:

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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Turofexorate Isopropyl (XL335) is a potent, selective FXR agonist with EC50 of 4 nM, highly selective versus other nuclear receptors, such as LXR, PPAR, ER and etc. Phase 1.
Targets
FXR [1]
4 nM(EC50)
In vitro

WAY-362450 binds to the ligand-binding domain (LBD) of human FXR. WAY-362450 resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450. WAY-362450 promotes transcription of the human BSEP, human SHP, and mouse IBABP genes utilizing reporter constructs with EC50 of 17, 230, and 33 nM, respectively in promoter assays. WAY-362450 at concentration of 1 μM significantly induces mRNAs encoding for BSEP, SHP, and IBABP in human cell cultures to 13-, 2-, and 20-fold, respectively. [1] WAY-362450 at concentration of 1 μM suppresses interleukin-6-induced CRP expression in human Hep3B hepatoma cells, and the inhibitory effect is attenuated when knockdown of FXR by short interfering RNA.

In vivo WAY-362450 administrated intravenously or orally at does of 3 mg/kg in rats with a protracted half-life of 25 h, modest volume of distribution, and low clearance of 3.3 L/kg. WAY-362450 administered orally at dose of 10 mg/kg in normal C57bl/6 mice for a period of 7 days significantly lowers triglycerides to 62.0 ± 6.4 mg/dL and total cholesterol to 78.1 ± 5.0 mg/dL. WAY-362450 administered orally at dose of 1 and 3 mg/kg daily for 6 weeks in LDLR−/− mice, triglycerides is lowered by 19% and 39%, respectively, total cholesterol is lowered by 23% and 50%, respectively and lesion formation by 18% and 36%, respectively. [1] WAY-362450 intraperitoneally administrated at dose of 30 mg/kg daily for 4 days in wild type C57BL/6 mice attenuates lipopolysaccharide-induced serum amyloid P component and serum amyloid A3 mRNA levels in the liver. [3] WAY-362450 orally administered at dose of 30 mg/kg/day for 4 weeks in adult male C57BL/6 mice reduces inflammatory cell infiltration and hepatic fibrosis, the reduction in inflammatory cell infiltration correlates with deceased serum levels of keratinocyte derived chemokine (mKC) and MCP 1 and decreased hepatic gene expression of MCP-1 and VCAM-1, and the reduction of hepatic fibrosis by WAY-362450 treatment corresponded to a reduction in hepatic gene expression of fibrosis markers. [3] WAY-362450 administrated orally at dose of 30mg/kg in LDLR−/− and apoE−/− mice blocks diet-induced hypertriglyceridemia and elevations of non-HDL cholesterol and produced a near complete inhibition of aortic lesion formation, WAY-362450 also induced small heterodimer partner (SHP) expression and repressed cholesterol 7α-hydroxylase (CYP7A1) and sterol 12 α-hydroxylase (CYP8B1) expression. [4]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Seven week old male C57bl/6 mice
  • Formulation: NMP:Solutol:PEG400:H2O, 10:10:40:40
  • Dosages: 10 mg/kg
  • Administration: Administrated orally once daily in the morning for a period of 7 days
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 33 mg/mL (75.26 mM) warming
Ethanol 2 mg/mL (4.56 mM)
Water <1 mg/mL
In vivo NMP+polyethylene glycol 300 (10+90, v+v) 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 438.47
Formula

C25H24F2N2O3

CAS No. 629664-81-9
Storage powder
in solvent
Synonyms Fxr 450

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00509756 Terminated Healthy Wyeth is now a wholly owned subsidiary of Pfizer November 2007 Phase 1
NCT00499629 Completed Healthy Wyeth is now a wholly owned subsidiary of Pfizer October 2007 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID