体外活性：厄贝沙坦与血管紧张素 II (AII) 竞争与 AT1 受体亚型的结合，并拮抗 AII 诱导的兔主动脉环收缩，IC50 为 4 nM。厄贝沙坦对 AT2 受体没有亲和力。厄贝沙坦 (10 μM) 阻断血管紧张素 II 诱导的大鼠心脏成纤维细胞中 αv、β1、β3 和 β5 整合素、骨桥蛋白和 α-肌动蛋白 mRNA 和蛋白水平的增加，导致细胞与细胞外基质 (ECM) 蛋白的附着减少。厄贝沙坦处理以浓度依赖性方式显着诱导 3T3-L1 细胞中脂肪形成标记基因脂肪蛋白 2 (aP2) 的表达，EC50 为 3.5 μM，在 10 μM 浓度下诱导作用为 3.3 倍。 Irbesartan (10 μM) 显着诱导过氧化物酶体增殖物激活受体-γ (PPARγ) 的转录活性达 3.4 倍，而与 AT1 受体阻断作用无关。厄贝沙坦 (~10 μM) 预处理通过以浓度依赖性方式阻断血管紧张素 II 内化，减少血管紧张素 II 诱导的大鼠血管平滑肌细胞凋亡。激酶测定：厄贝沙坦是一种高效、特异性的血管紧张素 II 1 型 (AT1) 受体拮抗剂，IC50 为 1.3 nM。细胞测定：厄贝沙坦处理以浓度依赖性方式显着诱导 3T3-L1 细胞中脂肪形成标记基因脂肪蛋白 2 (aP2) 的表达，EC50 为 3.5 μM，在 10 μM 浓度下诱导作用为 3.3 倍。 Irbesartan (10 μM) 显着诱导过氧化物酶体增殖物激活受体-γ (PPARγ) 的转录活性达 3.4 倍，而与 AT1 受体阻断作用无关。厄贝沙坦 (~10 μM) 预处理通过以浓度依赖性方式阻断血管紧张素 II 内化，减少血管紧张素 II 诱导的大鼠血管平滑肌细胞凋亡。

口服厄贝沙坦 (1 mg/kg) 可降低血管紧张素 II (AII) 诱导的高血压，在意识正常的血压大鼠中与氯沙坦等效，在血压正常的食蟹猴中明显比氯沙坦 (10 mg/kg) 更有效。厄贝沙坦（7 mg/kg/天）的给药可显着预防野百合碱诱导的充血性心力衰竭（CHF）大鼠的骨骼肌细胞凋亡和肌肉萎缩，这与 TNFα 水平的降低有关，并归因于 AT1 受体阻断。

厄贝沙坦是一种极强的选择性血管紧张素 II 1 型 (AT1) 受体拮抗剂，IC50 为 1.3 nM。

厄贝沙坦处理以浓度依赖性方式显着增加 3T3-L1 细胞中脂肪形成标记基因脂肪蛋白 2 (aP2) 的表达。浓度为 10 μM 时，诱导作用增加 3.3 倍，EC50 为 3.5 μM。即使没有阻断 AT1 受体的能力，厄贝沙坦 (10 μM) 仍可显着提高过氧化物酶体增殖物激活受体-γ (PPARγ) 的转录活性 3.4 倍。在大鼠血管平滑肌细胞中，厄贝沙坦 (~10 μM) 预处理可通过浓度依赖性方式抑制血管紧张素 II 内化，从而减少血管紧张素 II 诱导的细胞凋亡。

[1]. Irbesartan may relieve renal injury by suppressing Th22 cells chemotaxis and infiltration in Ang II-induced hypertension. Int Immunopharmacol . 2020 Oct:87:106789.

C25H29CLN6O

464.998

428.23

C, 64.58; H, 6.29; Cl, 7.62; N, 18.07; O, 3.44

329055-23-4

Irbesartan; 138402-11-6

Solid powder

CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5.Cl

ZUYFSRQJPNUOQU-UHFFFAOYSA-N

InChI=1S/C25H28N6O.ClH/c1-2-3-10-22-26-25(15-6-7-16-25)24(32)31(22)17-18-11-13-19(14-12-18)20-8-4-5-9-21(20)23-27-29-30-28-23;/h4-5,8-9,11-14H,2-3,6-7,10,15-17H2,1H3,(H,27,28,29,30);1H

2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one;hydrochloride

SR-47436; BMS 186295; BMS186295; SR47436; Avapro; Aprovel; KarveaIrbesartan HCl; Irbesartan hydrochloride; BMS-186295; SR 47436

2934.99.03.00

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。