2. Metabolic Enzyme/Protease
  3. Lipase
  4. XEN445

XEN445 is a potent, selective and orally active endothelial lipase (EL) inhibitor with an IC50 value of 0.237 μM. XEN445 selectively inhibits phospholipase enzymatic activity of LIPG. XEN445 raises plasma HDL and cholesterol levles. XEN445 induces G1 cell cycle arrest, reduces cell viability, suppresses cancer stem cell self-renewal, and inhibits tumor formation in LIPG-expressing triple-negative breast cancer cells, while showing no inhibitory effect on invasiveness or cancer stem cell stemness in these cells. XEN445 can be used for the research of cancer and metabolic disease, such as triple-negative breast cancer.

For research use only. We do not sell to patients.

XEN445

XEN445 Chemical Structure

CAS No. : 1515856-92-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

XEN445 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE XEN445

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

XEN445 is a potent, selective and orally active endothelial lipase (EL) inhibitor with an IC50 value of 0.237 μM. XEN445 selectively inhibits phospholipase enzymatic activity of LIPG. XEN445 raises plasma HDL and cholesterol levles. XEN445 induces G1 cell cycle arrest, reduces cell viability, suppresses cancer stem cell self-renewal, and inhibits tumor formation in LIPG-expressing triple-negative breast cancer cells, while showing no inhibitory effect on invasiveness or cancer stem cell stemness in these cells. XEN445 can be used for the research of cancer and metabolic disease, such as triple-negative breast cancer[1][2].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.25 μM
Compound: 13, XEN445
Inhibition of full length human endothelial lipase transfected in HEK293 cells using PED-A1 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
Inhibition of full length human endothelial lipase transfected in HEK293 cells using PED-A1 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
[PMID: 24211162]
In Vitro

XEN445 potently inhibits recombinant human endothelial lipase with an IC50 of 0.237 μM, and shows selectivity over human lipoprotein lipase ( IC50 = 20 μM) and human hepatic lipase ( IC50 = 9.5 μM)[1].
XEN445 (2.5 μM; 4 h) exhibits high binding to rat, mouse, and human plasma proteins, with 97.4%, 88.8%, and 95.4% binding respectively at 2.5 μM after 4 h at 37°C[1].
XEN445 potently inhibits recombinant human endothelial lipase-mediated hydrolysis of purified human HDL particles with an IC50 of 0.11 μM[1].
XEN445 (30 min) inhibits endothelial lipase activity in EL-transfected HEK-293 cells with an IC50 of 0.25 μM[1].
XEN445 (30 min) specifically inhibits LIPG phospholipase activity in parental and LIPG-overexpressing MDA-MB-468 cells, with an IC50 of 2.172 μM[2].
XEN445 (100-250 μM; 4 days) reduces viability of LIPG-expressing TNBC cells (MCF10DCIS, MDA-MB-468) via G1 cell cycle arrest in a LIPG-dependent manner[2].
XEN445 (250 μM; 3-4 days) enhances migration and invasion of LIPG-expressing TNBC cells (MDA-MB-468, MCF10DCIS)[2].
XEN445 (1 week) suppresses CSC self-renewal in LIPG-expressing TNBC cells (MCF10DCIS, MDA-MB-468)[2].
XEN445 upregulates expression of select stemness and EMT-related genes in LIPG-expressing TNBC cells (MDA-MB-468, MCF10DCIS)[2].

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

XEN445 Related Antibodies

Cell Viability Assay[2]

Cell Line: MCF10DCIS, MDA-MB-468, MCF7, T47D, LIPG-overexpressing MDA-MB-468, LIPG-knockdown MDA-MB-468, LIPG-overexpressing MCF7 cells
Concentration: 1, 2.5, 5, 10, 25, 50, 100, 200, 250 μM
Incubation Time: 4 days
Result: Reduced viability of MCF10DCIS cells at ≥100 μM.
Selectively reduced viability of LIPG-expressing TNBC cell lines (MCF10DCIS, MDA-MB-468) but not LIPG-negative luminal breast cancer cell lines (MCF7, T47D) at 200 and 250 μM.
Sensitized MDA-MB-468 and MCF7 cells to viability reduction via LIPG overexpression.
Rendered MDA-MB-468 cells resistant to viability reduction via LIPG knockdown.
Parmacokinetics
Species Dose Route AUC0-last CL Cmax Tmax T1/2 F
Mice[1] 10 mg/kg p.o. 253 μM·h / 62 μM 0.5 h 11.9 h 54 %
Mice[1] 1 mg/kg i.v. 47 μM·h 0.06 L/h/kg / / / /
In Vivo

XEN445 (30 mg/kg; i.g.,; b.i.d.; 3-9 days) increases plasma HDLc and total plasma cholesterol in wild-type male C57BL/6 mice[1].
XEN445 (50 mg/kg; i.p.; three times per week; 32 days) significantly inhibits in vivo triple-negative breast cancer xenograft tumor growth in nude mice were trans-
planted with MDA-MB-468 cells [2].

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

Animal Model: C57BL/6 (male, 12-16 weeks of age, wild-type)[1]
Dosage: 30 mg/kg
Administration: p.o.; b.i.d.; 3 or 9 days
Result: Increased total plasma cholesterol by 18% (from 106.1 mg/dL to 125.2 mg/dL) at 30 mg/kg for 3 days.
Increased plasma HDLc by 16% (from 74.7 mg/dL to 86.5 mg/dL) at 30 mg/kg for 3 days.
Increased total plasma cholesterol by 21% (from 108.3 mg/dL to 131.2 mg/dL) for 9 days.
Increased plasma HDLc by 30% (from 68.2 mg/dL to 88.7 mg/dL) for 9 days.
Animal Model: NU/NU (8-week-old female) trans-
planted with MDA-MB-468 cells[2]
Dosage: 50 mg/kg
Administration: i.p.; three times per week; 32 days
Result: Significantly inhibited tumor growth compared to vehicle control.
Reduced Ki67-positive cells to 150 ± 18 per 1000 tumor cells, representing a decrease compared to vehicle control's 423 ± 27 per 1000 tumor cells.
Showed no significant difference in vimentin staining compared to vehicle control.
Molecular Weight

366.33

Formula

C18H17F3N2O3
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[C@@H](OCC3=NC=CC=C3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (109.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7298 mL 13.6489 mL 27.2978 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
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Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7298 mL 13.6489 mL 27.2978 mL 68.2445 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 mL 13.6489 mL
10 mM 0.2730 mL 1.3649 mL 2.7298 mL 6.8244 mL
15 mM 0.1820 mL 0.9099 mL 1.8199 mL 4.5496 mL
20 mM 0.1365 mL 0.6824 mL 1.3649 mL 3.4122 mL
25 mM 0.1092 mL 0.5460 mL 1.0919 mL 2.7298 mL
30 mM 0.0910 mL 0.4550 mL 0.9099 mL 2.2748 mL
40 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7061 mL
50 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3649 mL
60 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1374 mL
80 mM 0.0341 mL 0.1706 mL 0.3412 mL 0.8531 mL
100 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
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XEN445 Related Classifications

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.

Keywords:

XEN4451515856-92-4XEN 445XEN-445Lipasecancer stem cellcoronary artery diseaseendothelial lipasebasal-like triple-negative breast cancerG1 cell cycle arrestHEK-293 cellsHDL-cholesterolLIPGtriple-negative breast cancer cellsmiceInhibitorinhibitorinhibit

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