Orlistat

製品コードS1629 バッチS162903

印刷

化学情報

Chemical Structure Synonyms Tetrahydrolipstatin,Ro 18-0647 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H53NO5
分子量 495.73 CAS No. 96829-58-2
Solubility (25°C)* 体外 DMSO 99 mg/mL (199.7 mM)
Ethanol 99 mg/mL (199.7 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.
in vitro Orlistat, an inhibitor of lipases and fatty acid synthase, is used orally for long-term treatment of obesity. Orlistat shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein[1].
in vivo Orlistat, administered by oral route, is minimally absorbed by the gastrointestinal tract and is able to prevent the absorption of a large percentage of lipids, thereby reducing lipid supply from outside sources[1]. Because of its extremely low oral bioavailability, the effects of Orlistat are largely confined to the gastrointestinal tract, where it inactivates pancreatic lipase. Therefore, the formulation and route of delivery would have to be changed to treat tumors of the breast, prostate, and so on. Orlistat halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice. A pharmacokinetic analysis of Orlistat (155 mg/kg) administered by i.p. injection showed peak blood levels to be ∼10 μM 2 h after dosing (data not shown). Beyond this time, blood levels of the drug decayed rapidly[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Jurkat CD4+ T cell leukemia cell line
濃度 2.5, 5, 10, 20, 40 μM
反応時間 2 days
実験の流れ

Leukemic cells were cultured in the presence of graded concentrations of orlistat for two days. Control cultures were exposed to DMSO alone at the concentration corresponding to that utilized for orlistat 40 μM. At the end of the in vitro treatment, leukemic cells were lysed and subjected to western blot (WB) analysis.
動物実験 動物モデル Nude mice (PC-3 xenograft tumor)
投薬量 240 mg/kg/day
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Histone malonylation is regulated by SIRT5 and KAT2A [ iScience, 2023, 26(3):106193] PubMed: 36879797
Gasdermin E mediates resistance of pancreatic adenocarcinoma to enzymatic digestion through a YBX1-mucin pathway [ Nat Cell Biol, 2022, 24(3):364-372] PubMed: 35292781
Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305] PubMed: 36203054
Analysis of the metabolic proteome of lung adenocarcinomas by reverse-phase protein arrays (RPPA) emphasizes mitochondria as targets for therapy [ Oncogenesis, 2022, 11(1):24] PubMed: 35534478
Controlling drug release by introducing lipase inhibitor within a lipid formulation [ Int J Pharm, 2022, 623:121958] PubMed: 35760262
Activation of CTHRC1 by HOXB9 Promotes Angiogenesis through Fatty Acid Metabolism in Lung Adenocarcinoma [ Rev Invest Clin, 2022, 75(2):63-75] PubMed: 37205792
Investigations into the use of enzyme inhibitors to control drug release for overdose prevention [ Monash University, 2022, ] PubMed: None
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4] PubMed: 34580494
LINC00842 inactivates transcription co-regulator PGC-1α to promote pancreatic cancer malignancy through metabolic remodelling [ Nat Commun, 2021, 12(1):3830] PubMed: 34158490
Brown adipocyte ATF4 activation improves thermoregulation and systemic metabolism [ Cell Rep, 2021, 36(12):109742] PubMed: 34551310

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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