| Bioactivity | Nelfinavir-d4 is deuterated labeled Nelfinavir (HY-15287). Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][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]。Nelfinavir (AG1341) (1-10 μM；48 小时) 抑制多发性骨髓瘤细胞的增殖[5]。 Nelfinavir 抑制 26S 胰凝乳蛋白酶样蛋白酶体活性，损害增殖并触发细胞凋亡骨髓瘤细胞系和新鲜浆细胞[5]。 Nelfinavir (1-10 μM；17 小时) 诱导多发性骨髓瘤细胞系凋亡[5]。 Nelfinavir (5 μM；0-24 小时) 降低 AKT 的磷酸化[5]。 Nelfinavir 激活 caspase-3 的裂解，降低 AKT 的磷酸化，STAT-3、ERK1/2，并激活未折叠蛋白反应系统的促凋亡通路[5]。 Nelfinavir 也是 SARS-CoV 3CL pro 抑制剂，IC50 为 35.93 μM[6]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Nelfinavir-d4 相关抗体: |
| In Vivo | Nelfinavir (AG1341) (75 mg/kg；腹腔注射；每周 5 天，持续 21 天) 减少 NOD/SCID 小鼠的多发性骨髓瘤细胞生长[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Formula | C32H41D4N3O4S |
| Molar Mass | 571.81 |
| 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]. Bono C, et al. The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiple myeloma cells in vitro and in vivo. Haematologica. 2012;97(7):1101‐1109. [3]. Mondal D, et al. Nelfinavir suppresses signaling and nitric oxide production by human aortic endothelial cells: protective effects of thiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90. [4]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [5]. Gills JJ, et al. Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that inducesendoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo. Clin Cancer Res. 2007 Sep 1;13(17):5183-94. [6]. Kaldor SW, et al. Nelfinavir mesylate (AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85. |