S81427 |
Lomitapide (mesylate) |
| MedMol | 98% |
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- 产品描述： Lomitapide mesylate(AEGR-733; BMS-201038) is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM. IC50 value: 8 nM [1] Target: MTP inhibitor Lomitapide is a small-molecule, microsomal triglyceride transfer protein (MTP) inhibitor, for the treatment of both familial and primary hypercholesterolemia. Oral, once-daily lomitapide will be targeted at patients resistant to HMG-CoA reductase inhibitors (statins) either due to abnormalities in liver function or to discontinuation because of muscle pain.
- 靶点： Microsomal Triglyceride Transfer Protein (MTP)
- 体外研究： Bayesian statistics was previously used as a tool to virtually screen USFDA approved drugs for predicted β-haematin (synthetic haemozoin) inhibition and in vitro antimalarial activity. Here, the experimental evaluation of nine of the highest ranked drugs, is reported, confirming the accuracy of the model by showing an overall 93% hit rate. Lapatinib, nilotinib, and lomitapide showed the best activity for inhibition of β-haematin formation and parasite growth and were found to inhibit haemozoin formation in the parasite, providing mechanistic insights into their mode of antimalarial action. Furthermore, the SBVS method correctly identified the three most important β-haematin inhibiting drugs identified in the USFDA set using the Bayesian model, namely lapatinib, nilotinib, and lomitapide. Lapatinib, nilotinib, and lomitapide were all found to increase the freely exchangeable haem, and decrease haemozoin in a dose dependent manner confirmed by an unpaired two tailed t-test relative to control, therefore confirming that these drugs inhibit cellular haemozoin formation (Figure 2). Reference: Molecules. 2020 Apr; 25(7): 1571. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7180468/
- 体内研究： To evaluate whether the new animal model in which ldlr mutant zebrafish are subjected to short-term (5 days) HCD feeding can be useful for drug screening, the effects of probucol, an antioxidant, and lomitapide, an MTP inhibitor, were tested on vascular lipid accumulation. Both probucol and lomitapide have been shown to exert antioxidant and MTP inhibitor properties, respectively, in zebrafish. As was expected, lomitapide decreased the plasma lipid levels in ldlr mutants, as assessed by ORO staining (Fig. 5A), by blocking their absorption in the intestine. Vascular lipid deposits were not decreased by probucol treatment but were significantly decreased by the treatment with lomitapide (Fig. 5B, C), suggesting that lipid levels, but not lipid oxidation, play a dominant role in early vascular lipid accumulation event in loss-of-function ldlr mutant larvae. Reference: J Lipid Res. 2018 Feb; 59(2): 391–399. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5794413/
- 参考文献：
1. Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. 2. Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52. 3. Perry CM. Lomitapide: a review of its use in adults with homozygous familial hypercholesterolemia. Am J Cardiovasc Drugs. 2013 Aug;13(4):285-96.
- 溶解性： 10 mM in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.266 ml 6.331 ml 12.661 ml 5 mM 0.253 ml 1.266 ml 2.532 ml 10 mM 0.127 ml 0.633 ml 1.266 ml 50 mM 0.025 ml 0.127 ml 0.253 ml
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