Bioactivity | Vancomycin-d10 (TFA) is a deuterated labeled Vancomycin[1]. Vancomycin is an antibiotic for the treatment of bacterial infections. |
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]。Vancomycin 是一种大分子糖肽类化合物,分子量为1450 Da[2]。Vancomycin 是一种独特的糖肽,在结构上与目前可用的任何抗生素都无关。它还具有抑制易感细菌细胞壁第二阶段合成的独特作用方式。Vancomycin 对多种革兰氏阳性菌具有活性,例如 Staphylococcus aureus, Staph. epidermidis, Str. agalactiae, Str. bovis, Str. mutans, viridans streptococci, enterococci[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Vancomycin-d10 TFA 相关抗体: |
In Vivo | Vancomycin 是一种大分子糖肽类化合物,分子量为1450 Da[2]。Vancomycin 是一种独特的糖肽,在结构上与目前可用的任何抗生素都无关。它还具有抑制易感细菌细胞壁第二阶段合成的独特作用方式。Vancomycin 对多种革兰氏阳性菌具有活性,例如 Staphylococcus aureus, Staph. epidermidis, Str. agalactiae, Str. bovis, Str. mutans, viridans streptococci, enterococci[3]。Vancomycin 可用于动物建模,构建动物肾损伤模型。Vancomycin 静脉内给药,标准输注时间至少为 1 小时,以尽量减少输注相关的不良反应。肌酐清除率正常的受试者,Vancomycin 的α-分布期为30分钟至1小时,β-消除半衰期为6-12小时。分布容积为 0.4–1 L/kg。Vancomycin 与蛋白质的结合范围为 10% 至 50%。影响 Vancomycin 整体活性的因素包括其组织分布、接种量和蛋白结合效应[2]。感染小鼠的 Vancomycin 处理与处理期间临床、腹泻和组织病理学评分以及存活率的改善有关[4]。万古霉素是一种经典的肾损伤造模试剂,通过诱导动物氧化应激相关的细胞凋亡来诱发疾病。通常使用大鼠和小鼠作为动物模型[5][6]。万古霉素诱导剂量参考[5][6]:(1) 模型动物:C57BL/6J雄性小鼠(6周)VIKI:400 mg/kg/day,i.p,7 天(2) 模型动物:雄性Sprague-Dawley(SD)大鼠(200-250g)VIKI:400 mg/kg/day,i.p,7 天 .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } 诱导肾损伤模型[5] 致病原理 Vancomycin 通过诱导动物氧化应激相关的细胞凋亡来诱发疾病。 具体造模方法 Mice: C57BL/6 • male • 6-week-old Administration: 400 mg/kg • ip • once daily for 7 weeks 造模成功指标 分子变化:诱导细胞凋亡和肾脏 Cr、BUN、MDA、IL-1β、IL-6、TNF-α 和 NF-κB 升高。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Formula | C70H67D10Cl2F6N9O28 |
Molar Mass | 1687.36 |
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]. Rybak MJ, et al. The pharmacokinetic and pharmacodynamic properties of vancomycin. Clin Infect Dis. 2006 Jan 1;42 Suppl 1:S35-9. [3]. Juan He, et al. Vitamin C reduces vancomycin-related nephrotoxicity through the inhibition of oxidative stress, apoptosis, and inflammation in mice. Ann Transl Med. 2021 Aug; 9(16): 1319. [4]. Watanakunakorn C, et al. Mode of action and in-vitro activity of vancomycin. J Antimicrob Chemother. 1984 Dec;14 Suppl D:7-18. [5]. Ping Yu, et al. N-acetylcysteine Ameliorates Vancomycin-induced Nephrotoxicity by Inhibiting Oxidative Stress and Apoptosis in the in vivo and in vitro Models. Int J Med Sci. 2022; 19(4): 740–752. [6]. Warren CA, et al. Vancomycin treatment's association with delayed intestinal tissue injury, clostridial overgrowth, and recurrence of Clostridium difficile infection in mice. Antimicrob Agents Chemother. 2013 Feb;57(2):689-96. |