| Description |
Bis-T-23 (AG1717), tyrphostin derivative, is an HIV-I integrase inhibitor. Bis-T-23 can promote actin-dependent dynamin oligomerization. Bis-T-23 can be used for the research of HIV and chronic kidney diseases (CKD)[1][2].
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| Related Catalog |
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| In Vitro |
Bis-T-23 (AG1717) (0.18 μM) 可抑制 HIV-1 整合酶[2]。 AG1717 (2 μM) 可抑制整合酶与底物的结合 DNA[2]。
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| In Vivo |
Bis-T-23 (1 ng) 靶向足细胞中肌动蛋白依赖性动力蛋白寡聚化，以促进正常的 GFB 功能[1]。 Bis-T-23 (i.p.; 20, 40 mg/kg) 通过改变肌动蛋白动力学改善蛋白尿[1]。 Bis-T-23 (i.p.; 20, 40 mg/kg) 在啮齿类动物的多种遗传和慢性肾小球疾病模型中改善或预防蛋白尿并减少系膜基质扩张[1]。 Animal Model: Sprague-Dawley rats (8 weeks old, males); Mice[1] Dosage: 20, 40 mg/kg; 40 mg/kg Administration: Intraperitoneal injection; signle, once for 6 consecutive days Result: Specifically reduced proteinuria on days 18 and 24. Caused a transient reduction of proteinuria (single dose) in PKCε KO mice. Completely prevented the onset of high-level proteinuria in the CD2AP KO mice. Significantly extended the lifespans of CD2AP KO mice. Led to improved glomerular histology with less mesangial matrix accumulation. Animal Model: Zebrafish[1] Dosage: 1 ng Administration: Injection Result: Promoted oligomerization of zebrafish Dyn2. Increased the number of focal adhesions (FAs) and stress fibers in cultured podocytes.
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| References |
[1]. Schiffer M, et al. Pharmacological targeting of actin-dependent dynamin oligomerization ameliorates chronic kidney disease in diverse animal models. Nat Med. 2015;21(6):601-609. [2]. Mazumder, A.,et al. Effects of Tyrphostins, Protein Kinase Inhibitors, on Human Immunodeficiency Virus Type 1 Integrase. Biochemistry, 1995, 34(46), 15111–15122.
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