Irbesartan

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Chemical Structure| 138402-11-6 同义名 : 厄贝沙坦 ;BMS-186295;SR-47436
CAS号 : 138402-11-6
货号 : A262974
分子式 : C25H28N6O
纯度 : 95%
分子量 : 428.529
MDL号 : MFCD00864464
存储条件：

Pure form Keep in dark place,Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

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].
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 <<
实验方案
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
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.