Bioactivity | Perindopril-d3 (erbumine) is deuterated labeled Perindopril (erbumine) (HY-B0130A). Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure[1][2][3][4]. |
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]。Perindopril erbumine (1 μM, 24 h) 改善 LPS (HY-D1056) 诱导的大鼠星形细胞瘤细胞系 (C6) 和小鼠小胶质细胞系(BV2) 中 AT2R 表达的减少和胶质增生[2]。Perindopril erbumine (1 μM, 24 h) 抑制LPS (HY-D1056) 诱导的大鼠星形细胞瘤细胞系 (C6) 和小鼠小胶质细胞系(BV2)中 IκBα 降解,NF-кB 核转位和 STAT3 活化[2]。Perindopril erbumine (1 μM, 24 h) 改善LPS (HY-D1056) 诱导的大鼠星形细胞瘤细胞系 (C6) 和小鼠小胶质细胞系(BV2) 中炎症因子释放失衡,抑制活性氧生成和亚硝酸盐释放[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Perindopril-d3 erbumine 相关抗体: |
In Vivo | Perindopril erbumine (0.1 mg/kg,灌胃,一次一次,连续 5 天) 对 LPS 诱导的大鼠神经炎症具有保护作用[2]。Perindopril erbumine (0.42 mg/kg ,口服,一次一次,连续 4 周) 联合黄芪丹参汤 (4.7 g/kg,口服,一次一次,连续 4 周) 减轻 adenine(HY-B0152) 诱导的大鼠慢性肾脏病 (CKD)[3]。Perindopril erbumine (0.4-1.5 mg/kg,口服,每天 1 次,持续 4-24 周) 对自发性高血压大鼠 (SHR) 的血压有持续性影响[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Formula | C23H40D3N3O5 |
Molar Mass | 444.62 |
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]. Bhat S A, et al. Angiotensin receptor blockade modulates NFκB and STAT3 signaling and inhibits glial activation and neuroinflammation better than angiotensin-converting enzyme inhibition [J]. Molecular neurobiology, 2016, 53: 6950-6967. [3]. Wei X, et al. Combination of perindopril erbumine and huangqi-danshen decoction protects against chronic kidney disease via sirtuin3/mitochondrial dynamics pathway [J]. Evidence-Based Complementary and Alternative Medicine, 2022, 2022. [4]. Afonso T, et al. Pharmacodynamic evaluation of 4 angiotensin‐converting enzyme inhibitors in healthy adult horses [J]. Journal of veterinary internal medicine, 2013, 27(5): 1185-1192. [5]. Thybo N K, et al. Dose-dependent effects of perindopril on blood pressure and small-artery structure [J]. Hypertension, 1994, 23(5): 659-666. |