Turofexorate Isopropyl (XL335)
Catalog No.S2694 Synonyms: Fxr 450
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.
Cited by 1 Publication
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(B) FXR agonists repressed β-Catenin mediated transcriptional activity. HEK293 cells were transfected with TOPflash reporter and pRLTK plasmid, and then treated with FXR agonists, GW4064 or WAY-36240, ranging from 1–4 μM. Luciferase activity was measured 12-24 hours post treatment. TOPflash/FOPflash activity was normalized to that of the controls.
Oncotarget, 2015, 6(6):4226-38.. Turofexorate Isopropyl (XL335) purchased from Selleck.
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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. | ||
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| Targets |
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| 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. |
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| 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] |
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Solubility (25°C)
| In vitro | DMSO | 33 mg/mL warmed (75.26 mM) |
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| Ethanol | 2 mg/mL (4.56 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): NMP+polyethylene glycol 300 (10+90, v+v) For best results, use promptly after mixing. |
30 mg/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 | 438.47 |
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| 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 |
| 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 |
| NCT00499629 | Completed | Healthy | Wyeth is now a wholly owned subsidiary of Pfizer | October 2007 | Phase 1 |
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