Lipofermata is an inhibitor of fatty acid transport (FATP) with IC50 of 4.84 μM in Caco-2 cells[2]. Lipofermata directly impacts tumor cell growth via modulation of FATP2, decreased de novo dihydroceramide synthesis[3]. Pharmacologic blockade of FATPs with the small-molecule inhibitor Lipofermata abrogates lipid transport into melanoma cells and reduces melanoma growth and invasion[4].
Lipofermata 细胞实验
Cell Line
Concentration
Treated Time
Description
References
primary human adipocytes
IC50 39.34 µM
15 minutes
To evaluate the efficacy of Lipofermata in inhibiting fatty acid uptake, results showed weaker inhibition in primary human adipocytes.
Biochem Pharmacol. 2015 Nov 1;98(1):167-81
hsHepG2
IC50 2.74 µM
15 minutes
To evaluate the efficacy of Lipofermata in inhibiting fatty acid uptake, results showed significant inhibition in hsHepG2 cells.
Biochem Pharmacol. 2015 Nov 1;98(1):167-81
hsCaco-2
IC50 6.09 µM
15 minutes
To evaluate the efficacy of Lipofermata in inhibiting fatty acid uptake, results showed significant inhibition in hsCaco-2 cells.
Biochem Pharmacol. 2015 Nov 1;98(1):167-81
rnINS-1E
IC50 4.65 µM
15 minutes
To evaluate the efficacy of Lipofermata in inhibiting fatty acid uptake, results showed significant inhibition in rnINS-1E cells.
Biochem Pharmacol. 2015 Nov 1;98(1):167-81
mmC2C12
IC50 5.67 µM
15 minutes
To evaluate the efficacy of Lipofermata in inhibiting fatty acid uptake, results showed significant inhibition in mmC2C12 cells.
Biochem Pharmacol. 2015 Nov 1;98(1):167-81
HCC1937
2 μM
48 hours
Evaluate the inhibitory effect of Lipofermata on HCC1937 cell proliferation, results showed IC50 values indicating Lipofermata effectively inhibited cell growth
J Cancer Res Clin Oncol. 2024 May 16;150(5):258
MCF7
1 μM
48 hours
Evaluate the inhibitory effect of Lipofermata on MCF7 cell proliferation, results showed IC50 values indicating Lipofermata effectively inhibited cell growth
J Cancer Res Clin Oncol. 2024 May 16;150(5):258
DLD-1
1.0 mM
5 minutes
Evaluate the effect of Lipofermata on [123I]BMIPP accumulation in DLD-1 cells, showing significant reduction
Int J Mol Sci. 2024 Jul 15;25(14):7747
LS180
1.0 mM
5 minutes
Evaluate the effect of Lipofermata on [123I]BMIPP accumulation in LS180 cells, showing significant reduction
Int J Mol Sci. 2024 Jul 15;25(14):7747
H441
1.0 mM
5 minutes
Evaluate the effect of Lipofermata on [123I]BMIPP accumulation in H441 cells, showing significant reduction
Int J Mol Sci. 2024 Jul 15;25(14):7747
HepG2 cells
10 μM
various time points (up to 4 hours)
To investigate the time-dependent effect of Lipofermata on dihydroceramide synthesis, results showed that VLC-NBD-dihydroceramide synthesis levels decreased over time but reverted to control levels after 4 hours.
J Biol Chem. 2022 Apr;298(4):101735
HepG2 cells
10 μM
1 hour
To investigate the effect of Lipofermata on dihydroceramide synthesis, results showed that Lipofermata decreased the levels of VLC- and LC-NBD-dihydroceramide synthesis in a concentration-dependent manner.
J Biol Chem. 2022 Apr;298(4):101735
Lipofermata 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 male mice
Oral
300 mg/kg
Single dose
To evaluate the inhibition of fatty acid absorption by Lipofermata, results showed that oral administration of Lipofermata significantly reduced plasma levels of 13C-oleate.
Biochem Pharmacol. 2015 Nov 1;98(1):167-81
Zebrafish
BRAFV600E driven transgenic zebrafish melanoma model
Intratumoral injection
5 μM
Once daily for 5 days
To assess the effect of Lipofermata on melanoma growth, results showed Lipofermata significantly reduced melanoma cell growth and lipid content
Cancer Discov. 2018 Aug;8(8):1006-1025
C57BL/6 mice
Unilateral ureteral obstruction (UUO) model
Intraperitoneal injection
50 mg/kg/day
Once daily for 7 days
To evaluate the effect of FATP2 inhibitor Lipofermata on UUO-induced renal fibrosis. Results showed that Lipofermata significantly reduced renal fibrosis and lipid accumulation.
Cell Death Dis. 2020 Nov 20;11(11):994
BALB/c mice
Breast cancer model
Intraperitoneal injection
2.5 mg/kg
Every other day for 2 weeks
Evaluate the inhibitory effect of Lipofermata on tumor growth in vivo, results showed Lipofermata significantly inhibited tumor growth
J Cancer Res Clin Oncol. 2024 May 16;150(5):258
C57BL/6 mice
B16F10 melanoma model
Intraperitoneal injection
2.5 mg/kg
Once daily for 2 weeks
To investigate the effect of FATP2 inhibitor lipofermata on lipid accumulation in MDSCs. Results showed that lipofermata treatment altered lipid species in MDSCs.
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