Losartan Potassium (DuP 753)是一种血管紧张素II受体拮抗剂（IC50=20nM）。
Cas No.:124750-99-8
Sample solution is provided at 25 µL, 10mM.
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Losartan Potassium (DuP 753) is an angiotensin II receptor antagonist (IC50=20nM). Losartan Potassium (DuP 753) works by selectively blocking the AT1 receptor of angiotensin II. Losartan Potassium (DuP 753) can be used for the treatment of hypertension and diabetic nephropathy[1-4].
In vitro, pretreatment of Vero E6 cells with Losartan Potassium (DuP 753) (1–100μM) for 1 hour, followed by infection with SARS-CoV-2 (MOI=0.01) and culture for 96 hours, Losartan Potassium (DuP 753) significantly reduced viral nucleoprotein levels and inhibited viral replication[5]. Pretreatment of MV3 cells with Losartan Potassium (DuP 753) (0.7μM) for 30 minutes, followed by treatment with ATII (100nM), Losartan Potassium (DuP 753) significantly inhibited NHE1 activity in the cells[6].
In vivo, Losartan Potassium (DuP 753) (5-50mg/kg; oral administration) was administered to Swiss mice with 5-FU-induced intestinal mucositis for 4 days. Losartan Potassium (DuP 753) significantly prevented the 5-FU-induced intestinal mucositis effects[7]. Losartan Potassium (DuP 753) (10mg/kg) was orally administered daily via drinking water to CD2F1 mice bearing C26 cells for 19 days. Losartan Potassium (DuP 753) prevented tumor-induced muscle mass loss, reduced tumor weight, attenuated myocardial interleukin-6 expression, improved cardiomyocyte calcium signaling, and increased cardiomyocyte contraction speed, contractile function, and blood pressure in tumor-bearing mice[8].
References:
[1] Sica DA, Gehr TW, Ghosh S. Clinical pharmacokinetics of Losartan Potassium (DuP 753). Clin Pharmacokinet. 2005;44(8):797-814.
[2] Burnier M. Angiotensin II type 1 receptor blockers. Circulation. 2001 Feb 13;103(6):904-12.
[3] Ashry O, Schnecko A, Clauss WG, et al. Evidence for expression and function of angiotensin II receptor type 1 in pulmonary epithelial cells. Respir Physiol Neurobiol. 2014 May 1;195:37-40.
[4] Saleh N, Cosarderelioglu C, Vajapey R, et al. Losartan Potassium (DuP 753) Mitigates Oxidative Stress in the Brains of Aged and Inflamed IL-10-/- Mice. J Gerontol A Biol Sci Med Sci. 2022 Sep 1;77(9):1784-1788.
[5] Nejat R, Sadr AS, Freitas B, et al. Losartan Potassium (DuP 753) Inhibits SARS-CoV-2 Replication in Vitro. J Pharm Pharm Sci. 2021;24:390-399.
[6] Olschewski DN, Hofschröer V, Nielsen N, et al. The Angiotensin II Type 1 Receptor Antagonist Losartan Potassium (DuP 753) Affects NHE1-Dependent Melanoma Cell Behavior. Cell Physiol Biochem. 2018;45(6):2560-2576.
[7] Oliveira MMB, de Araújo AA, Ribeiro SB, et al. Losartan Potassium (DuP 753) improves intestinal mucositis induced by 5-fluorouracil in mice. Sci Rep. 2021 Dec 1;11(1):23241.
[8] Stevens SC, Velten M, Youtz DJ, et al. Losartan Potassium (DuP 753) treatment attenuates tumor-induced myocardial dysfunction. J Mol Cell Cardiol. 2015 Aug;85:37-47.
Losartan Potassium (DuP 753)是一种血管紧张素II受体拮抗剂（IC50=20nM）。Losartan Potassium (DuP 753)可通过选择性阻断血管紧张素II的AT1受体发挥作用。Losartan Potassium (DuP 753)可用于高血压和糖尿病肾病的相关治疗[1-4]。
在体外，Losartan Potassium (DuP 753)（1–100μM）预处理Vero E6细胞1小时，随后以SARS-CoV-2（MOI=0.01）感染后培养96小时。Losartan Potassium (DuP 753)显著降低病毒核蛋白水平，同时抑制病毒复制[5]。Losartan Potassium (DuP 753)（0.7μM）预处理MV3细胞30分钟，随后以ATII（100nM）处理。Losartan Potassium (DuP 753)可显著抑制细胞中NHE1的活性[6]。
在体内，Losartan Potassium (DuP 753)（5-50mg/kg；口服）用于处理由5-FU诱导肠黏膜炎的Swiss小鼠，持续4天。Losartan Potassium (DuP 753)显著预防了5-FU诱导的肠黏膜炎效应[7]。Losartan Potassium (DuP 753)（10mg/kg）每日通过饮用水口服处理携带C26细胞的CD2F1小鼠，持续19天。Losartan Potassium (DuP 753)预防了肿瘤诱导的肌肉质量损失，减少了肿瘤重量，减轻了心肌白细胞介素-6表达，改善了心肌细胞钙信号传导，提高了心肌细胞收缩速度、收缩功能和肿瘤小鼠的血压[8]。
| Cell experiment [1]: | |
Cell lines | Vero E6 cells (African green monkey kidney cell line) |
Preparation Method | Vero E6 cells were plated at 2 x 10⁴ cells/well in a 96-well plate and incubated overnight at 37°C. Losartan Potassium (DuP 753) was prepared in DMEM to concentrations from 1μM to 100μM. For pre-infection treatment, cells were preincubated with Losartan Potassium (DuP 753) for 1 hour, then infected with SARS-CoV-2 at a MOI=0.01 for 1 hour. After infection, fresh Losartan Potassium (DuP 753)-containing media was added. For post-infection treatment, cells were first infected with SARS-CoV-2 at a MOI=0.01 for 1 hour, then Losartan Potassium (DuP 753)-containing media was added. Cells were incubated for 96 hours at 37°C, 5% CO₂. |
Reaction Conditions | 1-100μM; pre-incubation 1 hour, incubation 96 hours. |
Applications | Losartan Potassium (DuP 753) treatment showed a dose-dependent and significant reduction in SARS-CoV-2 replication. Pre-infection treatment reduced SARS-CoV-2 nuclear protein levels, and post-infection treatment decreased viral replication. The half-maximal effective concentration (EC₅₀) of Losartan Potassium (DuP 753) was 13.7μM for pre-infection treatment and 41μM for post-infection treatment. |
| Animal experiment [2]: | |
Animal models | Swiss mice (Mus musculus) |
Preparation Method | Intestinal mucositis was induced by a single intraperitoneal administration of 5-fluorouracil (5-FU; 450mg/kg). Losartan Potassium (DuP 753) or saline was orally administered 30min before 5-FU injection and daily for 4 days. On the 4th day, animals were euthanized and segments of small intestine were collected for analysis. |
Dosage form | 5, 25 or 50mg/kg; oral administration; daily for 4 days. |
Applications | Losartan Potassium (DuP 753) prevented 5-FU-induced intestinal mucositis effects including histopathological damage (shortened villi, loss of crypt architecture, inflammatory cell infiltration), partially rescued body weight loss, prevented leukopenia, decreased pro-inflammatory cytokine levels (TNF-α and IL-1β), reduced oxidative stress markers (MDA and GSH), and modulated mRNA expression of NF-κB p65, TWEAK and Fn14. |
References: | |
| Cas No. | 124750-99-8 | SDF | |
| 别名 | 氯沙坦钾; DuP-753 potassium | ||
| 化学名 | potassium;[2-butyl-5-chloro-3-[[4-[2-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol | ||
| Canonical SMILES | CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=N[N-]4)CO)Cl.[K+] | ||
| 分子式 | C22H23ClKN6O | 分子量 | 462.01 |
| 溶解度 | ≥ 21.35mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1645 mL | 10.8223 mL | 21.6446 mL |
| 5 mM | 432.9 μL | 2.1645 mL | 4.3289 mL |
| 10 mM | 216.4 μL | 1.0822 mL | 2.1645 mL |
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