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/ Irbesartan/伊贝沙坦

Irbesartan/伊贝沙坦 {[allProObj[0].p_purity_real_show]}

货号：A262974 同义名： 厄贝沙坦 / BMS-186295; SR-47436

Irbesartan是一种选择性和竞争性的非肽类 angiotensin II 拮抗剂，具有抗高血压作用。

Irbesartan/伊贝沙坦 化学结构 CAS号：138402-11-6
Irbesartan/伊贝沙坦 化学结构
CAS号：138402-11-6
Irbesartan/伊贝沙坦 3D分子结构
CAS号：138402-11-6
Irbesartan/伊贝沙坦 化学结构 CAS号：138402-11-6
Irbesartan/伊贝沙坦 3D分子结构 CAS号：138402-11-6
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Irbesartan/伊贝沙坦 纯度/质量文件 产品仅供科研

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Irbesartan/伊贝沙坦 生物活性

靶点

  • AT1 receptor

    AT1 receptor, IC50:1.3 nM
描述 Irbesartan is a long-acting angiotensin II receptor blocker with high selectivity and significant blockade of the AT1 receptor. Treating patients with hypertension alone or with type 2 diabetes and nephropathy using irbesartan can control hypertension, prolong life, and reduce costs in relation to existing alternatives [3]. Irbesartan (50 mg/Kg) reduced gastric ulcer index, gastric acidity, and ameliorated indomethacin-induced gastric mucosal apoptotic and inflammatory aberrations[4]. Moreover, a pre-treatment with 100 μM irbesartan significantly increased SOD(Superoxide Dismutase) activity and catalase expression of 15 and 25%, respectively, compared to hypoxic cells [5].

Irbesartan/伊贝沙坦 细胞实验

Cell Line
Concentration Treated Time Description References
GEM-resistant BxPC-3 cell line 1 μM 72 h Evaluate the effect of Irbesartan on GEM-resistant BxPC-3 cell line, results showed that Irbesartan significantly reversed GEM resistance. J Exp Clin Cancer Res. 2023 May 4;42(1):111.
PDAC organoids (PDO02#) 1 μM 72 h Evaluate the effect of Irbesartan on PDAC organoid apoptosis, results showed that the combined regimen significantly induced the expression of cleaved-caspase3 and cleaved-caspase7. J Exp Clin Cancer Res. 2023 May 4;42(1):111.
PDAC organoids (PDO01#) 1 μM 72 h Evaluate the effect of Irbesartan on PDAC organoid apoptosis, results showed that the combined regimen significantly induced the expression of cleaved-caspase3 and cleaved-caspase7. J Exp Clin Cancer Res. 2023 May 4;42(1):111.

Irbesartan/伊贝沙坦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID and BALB/c-nude mice PDOX mouse models and KPC genetically engineered mouse models Oral gavage 20 mg/kg Twice a week for 8 weeks Evaluate the therapeutic effect of Irbesartan in vivo on PDAC, results showed that the combination regimen significantly reduced tumor burden and prolonged survival. J Exp Clin Cancer Res. 2023 May 4;42(1):111.
Mice Ang II-induced vascular remodeling model Intragastric administration 30 mg/kg/d Every day for 2 weeks Irbesartan alleviated Ang II-induced vascular remodeling and hypertension Redox Biol. 2023 Nov;67:102893.
C57 mice Bleomycin-induced pulmonary fibrosis model Oral administration in drinking water 2 mg/kg For 4 weeks To evaluate the effect of irbesartan on exosome-induced pulmonary fibrosis. Results showed that irbesartan reversed the fibrotic features induced by exosomes and reduced the levels of Ang II and AT1R. Chin Med J (Engl). 2021 Sep 2;134(18):2175-2185.
Mice Akita/ACE2KO mice Oral 50 mg/kg/d Once daily for 1 month Treatment with irbesartan rescued the systolic dysfunction in Akita/ACE2KO mice, normalized altered signaling pathways, flow-mediated dilation, and the increased oxidative stress in the cardiovascular system. Circ Res. 2012 May 11;110(10):1322-35
C57BL/6J mice Cerebral malaria model Oral gavage 50 mg/kg/d Once daily until complete clearance of parasitemia (days 11-16 after infection) To investigate the protective effect of Irbesartan as adjunctive therapy for cerebral malaria, results showed that Irbesartan significantly increased survival rates in mice. J Clin Invest. 2016 Oct 3;126(10):4016-4029
Mice BAPN-induced thoracic aortopathy model Oral 50 mg/kg/day Once daily for 4 weeks To evaluate the effect of irbesartan on BAPN-induced thoracic aortopathies; results showed irbesartan did not ameliorate aortic rupture and dilatation Arterioscler Thromb Vasc Biol. 2022 Oct;42(10):1254-1261

Irbesartan/伊贝沙坦 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00741702 Hypertension ... 展开 >>Diabetes Mellitus 收起 << Not Applicable Completed - -
NCT01195818 Sickle Cell Disease Not Applicable Completed - France ... 展开 >> Centre de la Drépanocytose, Service de Médecine Interne. Hôpital Tenon, 4 Rue de la Chine Paris, France, 75020 收起 <<
NCT01715207 Marfan Syndrome Phase 3 Completed - Korea, Republic of ... 展开 >> Samsung Medical Center Seoul, Korea, Republic of, 135-710 收起 <<

Irbesartan/伊贝沙坦 参考文献

[1]Kawano H, Cody RJ, et al. Angiotensin II enhances integrin and alpha-actinin expression in adult rat cardiac fibroblasts. Hypertension. 2000 Jan;35(1 Pt 2):273-9.

[2]Bernhart CA, Perreaut PM, et al. A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists. J Med Chem. 1993 Oct 29;36(22):3371-80.

[3]Gialama F, Maniadakis N. Comprehensive overview: efficacy, tolerability, and cost-effectiveness of irbesartan. Vasc Health Risk Manag. 2013;9:575-92. doi: 10.2147/VHRM.S50831. Epub 2013 Oct 7. PMID: 24124375; PMCID: PMC3794869.

[4]Shahin NN, Abdelkader NF, Safar MM. A Novel Role of Irbesartan in Gastroprotection against Indomethacin-Induced Gastric Injury in Rats: Targeting DDAH/ADMA and EGFR/ERK Signaling. Sci Rep. 2018 Mar 9;8(1):4280. doi: 10.1038/s41598-018-22727-6. PMID: 29523851; PMCID: PMC5844881.

[5]Boccellino M, Di Domenico M, Donniacuo M, Bitti G, Gritti G, Ambrosio P, Quagliuolo L, Rinaldi B. AT1-receptor blockade: Protective effects of irbesartan in cardiomyocytes under hypoxic stress. PLoS One. 2018 Oct 24;13(10):e0202297. doi: 10.1371/journal.pone.0202297. PMID: 30356256; PMCID: PMC6200178.

Irbesartan/伊贝沙坦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.67mL

2.33mL

1.17mL

23.34mL

4.67mL

2.33mL

Irbesartan/伊贝沙坦 技术信息

CAS号138402-11-6
分子式C25H28N6O
分子量 428.53
SMILES Code C3=C(CN1C(=O)C2(N=C1CCCC)CCCC2)C=CC(=C3)C4=CC=CC=C4C5=N[NH]N=N5
MDL No. MFCD00864464
别名 厄贝沙坦 ;BMS-186295; SR-47436
运输蓝冰
InChI Key YOSHYTLCDANDAN-UHFFFAOYSA-N
Pubchem ID 3749
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, room temperature
溶解方案

DMSO: 105 mg/mL(245.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Irbesartan | 138402-11-6 | SR-47436 | BMS-186295 | SR47436 | SR 47436 | BMS186295 | BMS 186295 | BMS-186295 | Angiotensin Receptor Antagonist | GPCR/G Protein | Apoptosis | Angiotensin Receptor | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Irbesartan/伊贝沙坦 纯度/质量文件 | Irbesartan/伊贝沙坦 生物活性 | Irbesartan/伊贝沙坦 临床数据 | Irbesartan/伊贝沙坦 参考文献 | Irbesartan/伊贝沙坦 实验方案 | Irbesartan/伊贝沙坦 技术信息

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