Irbesartan是一种血管紧张素II受体（AT1）拮抗剂。
Cas No.:138402-11-6
Sample solution is provided at 25 µL, 10mM.
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Irbesartan is an angiotensin II receptor (AT1) antagonist. Irbesartan downregulates the binding of angiotensin II to the AT1 receptor, thereby participating in the modulation of various signaling pathways. Irbesartan can be used in studies related to hypertension and diabetic nephropathy in type 2 diabetes[1-4].
In vitro, gemcitabine-resistant pancreatic cancer cells (PANC-1, L3.7, MiaPaca-2, SW1990) were treated with Irbesartan (1μM) and gemcitabine (0.8μM) for 72 hours. Irbesartan significantly inhibited the expression of c-Jun, SOX9, SOX2, OCT4, FTH1, FTL, and TFRC, while reducing gemcitabine resistance and tumor stemness[5]. Irbesartan (10μM) was pre-incubated with 3T3-L1 adipocytes for 1.5 hours, followed by stimulation with Ang III (10nM) for 12 hours. Irbesartan failed to inhibit the increase in glucose uptake and the upregulation of GLUT1 expression[6].
In vivo, Irbesartan (20mg/kg/day) was orally administered to spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats for 14 days. Irbesartan significantly protected SHR rats from hypertension-induced cognitive dysfunction[7]. Irbesartan (40mg/kg/day; once daily) was administered intranasally to male APP/PS1 mice for 10 weeks. Irbesartan significantly improved the memory performance of the mice and reduced neurodegeneration, oxidative stress, and neuroinflammation[8].
References:
[1] Schupp M, Janke J, Clasen R, et al. Angiotensin type 1 receptor blockers induce peroxisome proliferator-activated receptor-gamma activity. Circulation. 2004 May 4;109(17):2054-7.
[2] Ruiz E, Redondo S, Padilla E, et al. Importance of intracellular angiotensin II in vascular smooth muscle cell apoptosis: inhibition by the angiotensin AT1 receptor antagonist irbesartan. Eur J Pharmacol. 2007 Jul 19;567(3):231-9.
[3] Zhong Y, Tang R, Lu Y, et al. Irbesartan may relieve renal injury by suppressing Th22 cells chemotaxis and infiltration in Ang II-induced hypertension. Int Immunopharmacol. 2020 Oct;87:106789.
[4] Vanderheyden PM, Fierens FL, De Backer JP, et al. Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors. Br J Pharmacol. 1999 Feb;126(4):1057-65.
[5] Zhou T, Xie Y, Hou X, et al. Irbesartan overcomes gemcitabine resistance in pancreatic cancer by suppressing stemness and iron metabolism via inhibition of the Hippo/YAP1/c-Jun axis. J Exp Clin Cancer Res. 2023 May 4;42(1):111.
[6] Tanioka T, Maeda K, Takahashi R, et al. The Ang III/AT2R Pathway Enhances Glucose Uptake by Improving GLUT1 Expression in 3T3-L1 Adipocytes. Biol Pharm Bull. 2021;44(7):1014-1018.
[7] Hao S, He Q, Yuan Y, et al. The protective effects of Irbesartan in cognitive impairment in hypertension. Aging (Albany NY). 2024 Mar 23;16(6):5065-5076.
[8] Gouveia F, Pérez MC, Bicker J, et al. Protective effects of irbesartan against neurodegeneration in APP/PS1 mice: Unraveling its triple anti-apoptotic, anti-inflammatory and anti-oxidant action. Biomed Pharmacother. 2025 Jul;188:118167.
Irbesartan是一种血管紧张素II受体（AT1）拮抗剂。Irbesartan可下调血管紧张素II与AT1受体的结合，来参与多种信号通路的调节。Irbesartan可用于高血压和2型糖尿病肾病的相关研究[1-4]。
在体外，Irbesartan（1μM）gemcitabine（0.8μM）刺激gemcitabine耐药的胰腺癌细胞（PANC-1，L3.7，MiaPaca-2，SW1990）72小时。Irbesartan显著抑制c-Jun、SOX9、SOX2、OCT4、FTH1、FTL及TFRC的表达，同时降低gemcitabine耐药和肿瘤干性[5]。Irbesartan（10μM）预处理3T3-L1脂肪细胞1.5小时，随后以Ang III（10nM）刺激12小时。Irbesartan未能抑制葡萄糖摄取的增加及GLUT1的表达上调[6]。
在体内，Irbesartan（20mg/kg/day）口服灌胃于自发性高血压（SHR）大鼠和Wistar-Kyoto（WKY）大鼠14天。Irbesartan显著保护了SHR大鼠免受高血压诱导的认知功能障碍[7]。Irbesartan（40mg/kg/day；每日一次）鼻内给药于APP/PS1雄性小鼠10周。Irbesartan显著改善了小鼠的记忆表现，减少了神经退行性病变、氧化应激与神经炎症[8]。
| Cell experiment [1]: | |
Cell lines | PDAC cell lines (e.g., PANC-1, L3.7, MiaPaca-2, SW1990) and low-passage primary PDAC cells |
Preparation Method | Cells were maintained in DMEM or RPMI 1640 basal medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin solution at 37°C in a humidified atmosphere of 95% air and 5% CO₂. Cells were treated with Irbesartan (1μM) alone or in combination with Gemcitabine (GEM). |
Reaction Conditions | 1μM; 72h |
Applications | Irbesartan effectively overcame gemcitabine resistance in PDAC cells. Irbesartan synergistically enhanced the cytotoxicity of Gemcitabine, significantly reducing cell viability and inducing cellular apoptosis. Irbesartan suppressed the stemness properties of PDAC cells by inhibiting sphere formation and reducing the population of cancer stem cells (CSCs) expressing markers such as ESA+CD24+CD44+, ALDH+, and CD133+. Irbesartan altered cellular iron metabolism by affecting the labile iron pool. Irbesartan inhibited the Hippo/YAP1 signaling pathway, which subsequently decreased c-Jun expression and downregulated its downstream target genes involved in stemness (SOX9, SOX2, OCT4) and iron metabolism (FTH1, FTL, TFRC). |
| Animal experiment [2]: | |
Animal models | APP/PS1 transgenic mice (male) |
Preparation Method | Mice were intranasally administered Irbesartan (40mg/kg/day) formulated in a thermoreversible gel for 10 weeks, starting at 4 months of age. Behavioral, histological, and biochemical analyses were performed at the end of the treatment period. |
Dosage form | 40mg/kg/day; intranasal; daily administration for 10 weeks |
Applications | Irbesartan treatment significantly improved memory performance, enhanced dendritic spine density, restored mitochondrial bioenergetics and blood-brain barrier (BBB) integrity, and reduced apoptotic, oxidative, and neuroinflammatory markers. |
References: | |
| Cas No. | 138402-11-6 | SDF | |
| 别名 | 厄贝沙坦; SR-47436; BMS-186295 | ||
| 化学名 | 2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one | ||
| Canonical SMILES | CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5 | ||
| 分子式 | C25H28N6O | 分子量 | 428.53 |
| 溶解度 | 100mg/ml in DMSO (Need ultrasonic),≥1149 mg/mL in EtOH with ultrasonic | 储存条件 | Store at RT |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3336 mL | 11.6678 mL | 23.3356 mL |
| 5 mM | 466.7 μL | 2.3336 mL | 4.6671 mL |
| 10 mM | 233.4 μL | 1.1668 mL | 2.3336 mL |
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