XEN445
CAS No. : 1515856-92-4
| Size | Price | Stock |
|---|---|---|
| 5mg | $46 | In-stock |
| 10mg | $75 | In-stock |
| 25mg | $150 | In-stock |
| 50mg | $240 | In-stock |
| 100mg | $390 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-12246 |
| M.Wt: | 366.33 |
| Formula: | C18H17F3N2O3 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 40 mg/mL |
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].
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].
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].
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