Lomitapide | Microsomal triglyceride transfer protein inhibitor
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $49.00 | ||
| 25 mg | $195.00 |
Lomitapide (182431-12-5) is a potent (IC50 = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia.1,2 It has displayed anticancer activity acting through various pathways including autophagy-dependent cancer cell death via direct inhibition of the kinase activity of mTORC13, activation of AMPK/Beclin1-mediated autophagy4, Notch inhibition via targeting TACE and γ-secretase5, blocking ZDHHC5-dependent palmitoylation on SSTR56, PFKFB3 inhibition7, and PARP14/DRP1-mediated mitophagy8.
References/Citations:
- Wetterau et al. (1998), An MTP Inhibitor That Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits; Science 282 751
- Cuchel et al. (20013), Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolemia: a single-arm, open-label, phase 3 study; Lancet 381 40
- Lee et al. (2022), Lomitapide, a cholesterol-lowering drug, is an anticancer agent that induces autophagic cell death via inhibiting mTOR; Cell Death Dis. 13 603
- Zuo et al. (2021), Targeting PP2A with lomitapide suppresses colorectal tumorigenesis through activation of AMPK/Beclin1-mediated autophagy; Cancer Lett. 521 281
- Kandasamy and Ghosh (2023), Multi-targeting TACE/ADAM17 and gamma-secretase of notch signaling pathway in TNBC via drug repurposing approach using Lomitapide; Cell Signal. 102 110529
- Wang et al. (2023), Repositioning Lomitapide to block ZDHHC5-dependent palmitoylation on SSTR5 leads to anti-proliferation effect in preclinical pancreatic cancer models; Cell Death Discov. 9 60
- Cao et al. (2024), Drug-repurposing by virtual and experimental screening of PFKFB3 inhibitors for pancreatic cancer therapy; Eur. J. Pharmacol. 965 176330
- Zhang et al. (2024), Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma; Cancer Lett. Online ahead of print 216802
C39H37F6N3O2
>98% by HPLC
NMR: Conforms
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Lomitapide (182431-12-5) is a potent (IC50 = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia.1,2 It has displayed anticancer activity acting through various pathways including autophagy-dependent cancer cell death via direct inhibition of the kinase activity of mTORC13, activation of AMPK/Beclin1-mediated autophagy4, Notch inhibition via targeting TACE and γ-secretase5, blocking ZDHHC5-dependent palmitoylation on SSTR56, PFKFB3 inhibition7, and PARP14/DRP1-mediated mitophagy8.
References/Citations:
- Wetterau et al. (1998), An MTP Inhibitor That Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits; Science 282 751
- Cuchel et al. (20013), Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolemia: a single-arm, open-label, phase 3 study; Lancet 381 40
- Lee et al. (2022), Lomitapide, a cholesterol-lowering drug, is an anticancer agent that induces autophagic cell death via inhibiting mTOR; Cell Death Dis. 13 603
- Zuo et al. (2021), Targeting PP2A with lomitapide suppresses colorectal tumorigenesis through activation of AMPK/Beclin1-mediated autophagy; Cancer Lett. 521 281
- Kandasamy and Ghosh (2023), Multi-targeting TACE/ADAM17 and gamma-secretase of notch signaling pathway in TNBC via drug repurposing approach using Lomitapide; Cell Signal. 102 110529
- Wang et al. (2023), Repositioning Lomitapide to block ZDHHC5-dependent palmitoylation on SSTR5 leads to anti-proliferation effect in preclinical pancreatic cancer models; Cell Death Discov. 9 60
- Cao et al. (2024), Drug-repurposing by virtual and experimental screening of PFKFB3 inhibitors for pancreatic cancer therapy; Eur. J. Pharmacol. 965 176330
- Zhang et al. (2024), Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma; Cancer Lett. Online ahead of print 216802
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