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MedChemExpress - Model Orlistat-d3 - ...

MedChemExpress - Model Orlistat-d3 - 1356930-46-5

Orlistat-d3 is a deuterated labeled Orlistat[1]. Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity[2].?Anti-atherosclerotic?effect[3].

Orlistat-d3

MCE China：Orlistat-d3

Brand：MedChemExpress (MCE)

Cat. No.HY-B0218S

CAS：1356930-46-5

Synonyms：Tetrahydrolipstatin-d3; Ro-18-0647-d3

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Orlistat-d3 is a deuterated labeled Orlistat. Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity.?Anti-atherosclerotic?effect.

In Vitro：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].Orlistat (40 μM; 2 days) does not affect MGMT levels in a human melanoma cell line, but downregulates the repair protein by 30-70% in human peripheral blood mononuclear cells, in two leukemia and two colon cancer cell lines. Orlistat does not alter noticeably MGMT mRNA expression[2].

In Vivo：Orlistat (10 mg/kg/day) significantly improves lipid profile, increases antioxidant enzymes and expression of anti-inflammatory markers, and decreases the expression of the pro-inflammatory marker compared to the obese (OB) group[3].

References：

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]

[2]. Giorgia Cioccoloni, et al. Influence of fatty acid synthase inhibitor orlistat on the DNA repair enzyme O6-methylguanine-DNA methyltransferase in human normal or malignant cells in vitro. Int J Oncol. 2015 Aug;47(2):764-72. [Content Brief]

[3]. Zaidatul Akmal Othman, et al. Anti-Atherogenic Effects of Orlistat on Obesity-Induced Vascular Oxidative Stress Rat Model. Antioxidants (Basel). 2021 Feb 6;10(2):251. [Content Brief]

Brand introduction:
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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