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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 血管紧张素受体 / Olmesartan medoxomil/奥美沙坦酯

Olmesartan medoxomil/奥美沙坦酯 {[allProObj[0].p_purity_real_show]}

货号：A131632 同义名： CS 866

Olmesartan medoxomil是一种合成的咪唑类衍生血管紧张素II受体拮抗剂，作为前药具有抗高血压特性。

Olmesartan medoxomil/奥美沙坦酯 化学结构 CAS号：144689-63-4
Olmesartan medoxomil/奥美沙坦酯 化学结构
CAS号：144689-63-4
Olmesartan medoxomil/奥美沙坦酯 3D分子结构
CAS号：144689-63-4
Olmesartan medoxomil/奥美沙坦酯 化学结构 CAS号：144689-63-4
Olmesartan medoxomil/奥美沙坦酯 3D分子结构 CAS号：144689-63-4
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Olmesartan medoxomil/奥美沙坦酯 纯度/质量文件 产品仅供科研

货号：A131632 标准纯度： {[allProObj[0].p_purity_real_show]}
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Olmesartan medoxomil/奥美沙坦酯 生物活性

描述 Inhibition of Arachidonic acid (AA) metabolism by angiotensin II receptor blockers (ARBs) occurs in a concentration-dependent manner, with Olmesartan showing an IC50 of 66.2 μM[1]. Olmesartan medoxomil is identified as a potent, selective blocker of the angiotensin AT1 receptor[2].
体内研究

The effectiveness of Olmesartan was evaluated in db/db diabetic mice over a 12-week period, starting from weeks 10 to 22 of age. These mice exhibited a significant increase in albuminuria (11.7-fold) compared to controls. Treatment with Olmesartan for twelve weeks notably reduced albuminuria by 77% versus placebo, and the albumin/creatinine ratio (ACR) saw a significant decrease by 59% in treated db/db mice, highlighting its potential benefits in diabetic conditions[3].
体外研究

Inhibition of Arachidonic acid (AA) metabolism by angiotensin II receptor blockers (ARBs) occurs in a concentration-dependent manner, with Olmesartan showing an IC50 of 66.2 μM[1].

Olmesartan medoxomil is identified as a potent, selective blocker of the angiotensin AT1 receptor[2].

Olmesartan medoxomil/奥美沙坦酯 细胞实验

Cell Line
Concentration Treated Time Description References
Primary osteocytes 10 mM 120 min Olmesartan medoxomil ameliorated angiotensin II-induced impairment of cell viability and ROS production. J Bone Miner Res. 2021 Jan;36(1):67-79.
vascular smooth muscle cells (VSMCs) 100 nM 20 min To evaluate the effect of angiotensin (1–7) on Trail-induced Jnk phosphorylation and Mmp9 expression, results showed that angiotensin (1–7) effectively decreased Trail-induced Jnk phosphorylation and attenuated the upregulation of Mmp9 mRNA expression. J Am Heart Assoc. 2023 Feb 7;12(3):e027589.

Olmesartan medoxomil/奥美沙坦酯 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats TNBS-induced acute colitis Oral 3.0 and 10.0 mg/kg Once daily for 7 days The study aimed to investigate the effects of OM self-microemulsifying drug delivery system (OMS) in TNBS-induced acute colitis in rats. Results showed that OMS, compared with OM, dose-dependently achieved higher colonic free olmesartan concentration, showed better anti-inflammatory, antioxidant, and anti-apoptotic effects, improved intestinal barrier, and decreased mucolytic activity. Drug Deliv. 2022 Dec;29(1):2017-2028
Mice Dbb mice Oral gavage 10 mg/kg and 20 mg/kg Once daily for 8 weeks To evaluate the effects of olmesartan medoxomil on the progression of diabetic nephropathy and renal function in dbb mice. The results showed that olmesartan medoxomil improved the physiological and biochemical parameters in dbb mice, decreased urinary albumin excretion and plasma creatinine levels, and reduced glomerular and tubular injury, suggesting that olmesartan medoxomil improved renal function and minimized renal pathological deterioration in dbb mice. Drug Des Devel Ther. 2019 Oct 22;13:3657-3667
Mice ApoE-null mouse model Subcutaneous infusion 1.4 μM/g 28 days To evaluate the effect of Olmesartan medoxomil in preventing aortic aneurysm, results showed that co-infusion of Olmesartan medoxomil with TRV027 prevented the development of aortic aneurysm through distinct mechanisms. Hypertension. 2023 Feb;80(2):385-402
Rats Nephrectomized model Osmotic pump 3 mg/kg Every 2 weeks for 6 weeks Olmesartan medoxomil partially improved the bone elastic mechanical properties and chemical composition in nephrectomized rats, suppressing osteocyte apoptosis and skeletal pentosidine accumulation. J Bone Miner Res. 2021 Jan;36(1):67-79.
Mice Opg-KO mice Oral 20 mg/kg Starting 2 weeks before AAA induction to the date of euthanasia To evaluate the protective effect of olmesartan on AAA progression in Opg-KO mice, results showed that olmesartan prevented AAA progression by upregulating angiotensin (1–7), attenuating excessive aortic dilatation and collapse of tunica media. J Am Heart Assoc. 2023 Feb 7;12(3):e027589.
Mice Pregnancy-associated hypertensive (PAH) mouse model Oral 15 mg/l From pregnancy day 13 to day 19 To investigate the effect of Olmesartan on cardiac hypertrophy in PAH mice, results showed that Olmesartan restored Adra1a mRNA expression levels J Biol Chem. 2023 Mar;299(3):102964
Nude mice Bladder cancer xenograft model Oral 10 mg/kg Once daily for 14 days To evaluate the efficacy of ARB olmesartan in suppressing the growth of platinum-resistant bladder cancer xenograft models. Results showed that olmesartan significantly suppressed the growth of T24PR tumours. Br J Cancer. 2011 Oct 25;105(9):1331-7
Mice Anti-glomerular basement membrane antibody-induced glomerulonephritis model Oral 6 mg/kg Once daily, continued until Day 7 To evaluate the inhibitory effects of Olmesartan medoxomil on glomerular lesions in Tg mice, results showed that Olmesartan significantly improved proteinuria and glomerular pathological changes in Tg mice. Nephrol Dial Transplant. 2011 Nov;26(11):3465-73
CD-1 mice 5/6 nephrectomy model Diet administration 100 mg/kg Daily for 4 weeks Olmesartan significantly slowed the progression of chronic kidney disease in CD-1 mice following 5/6 nephrectomy, reducing blood pressure, albuminuria, loss of renal function, and glomerular and tubular injury. Kidney Int. 2010 Dec;78(11):1136-53

Olmesartan medoxomil/奥美沙坦酯 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
NCT01271374 Hypertension Phase 4 Unknown December 2011 United States, Georgia ... 展开 >> Atlanta Clinical Research Center Tucker, Georgia, United States, 30084 收起 <<
NCT01870739 - Completed - -
NCT02089399 Healthy Phase 1 Completed - Korea, Republic of ... 展开 >> Samsung medical center Seoul, Korea, Republic of 收起 <<

Olmesartan medoxomil/奥美沙坦酯 参考文献

[1]Senda A, et al. Effects of Angiotensin II Receptor Blockers on Metabolism of Arachidonic Acid via CYP2C8. Biol Pharm Bull. 2015;38(12):1975-9.

[2]Shah S, et al. Simultaneous Quantitative Analysis of Olmesartan Medoxomil and Amlodipine Besylate in Plasma by High-performance Liquid Chromatography Technique. J Young Pharm. 2012 Apr;4(2):88-94.

[3]Gu J, et al. Olmesartan Prevents Microalbuminuria in db/db Diabetic Mice Through Inhibition of Angiotensin II/p38/SIRT1-Induced Podocyte Apoptosis. Kidney Blood Press Res. 2016 Nov 21;41(6):848-864.

Olmesartan medoxomil/奥美沙坦酯 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.79mL

0.36mL

0.18mL

8.95mL

1.79mL

0.90mL

17.90mL

3.58mL

1.79mL

Olmesartan medoxomil/奥美沙坦酯 技术信息

CAS号144689-63-4
分子式C29H30N6O6
分子量 558.59
SMILES Code C3=C(C[N]1C(=C(N=C1CCC)C(O)(C)C)C(OCC2=C(OC(O2)=O)C)=O)C=CC(=C3)C5=C(C4=N[NH]N=N4)C=CC=C5
MDL No. MFCD00944911
别名 CS 866
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(89.51 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: Olmesartan medoxomil | 144689-63-4 | CS 866 | CS866 | CS-866 | Angiotensin Receptor Inhibitor | GPCR/G Protein | Angiotensin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Olmesartan medoxomil/奥美沙坦酯 纯度/质量文件 | Olmesartan medoxomil/奥美沙坦酯 生物活性 | Olmesartan medoxomil/奥美沙坦酯 临床数据 | Olmesartan medoxomil/奥美沙坦酯 参考文献 | Olmesartan medoxomil/奥美沙坦酯 实验方案 | Olmesartan medoxomil/奥美沙坦酯 技术信息

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