受注:045-509-1970 |
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Synonyms | Tetrahydrolipstatin,Ro 18-0647 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C29H53NO5 |
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分子量 | 495.73 | CAS No. | 96829-58-2 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (201.72 mM) | |
Ethanol | 100 mg/mL (201.72 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. |
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. |
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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]. |
細胞アッセイ | 細胞株 | Jurkat CD4+ T cell leukemia cell line |
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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. |
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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. |
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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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。