Bioactivity | 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]. |
Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。Orlistat (40 μM;2 天) 不影响人黑色素瘤细胞系中的 MGMT 水平,但在人外周血单核细胞、两种白血病和两种结肠癌细胞系中下调修复蛋白 30-70%。Orlistat 不会显著改变 MGMT mRNA 表达[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Orlistat-d3 相关抗体: |
In Vivo | 与肥胖 (OB) 组相比,Orlistat (10 mg/kg/天) 显著改善血脂状况,增加抗氧化酶和抗炎标志物的表达,并降低促炎标志物的表达[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 1356930-46-5 |
Formula | C29H50D3NO5 |
Molar Mass | 498.75 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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. [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. |