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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 / Fimasartan/非马沙坦

Fimasartan/非马沙坦 {[allProObj[0].p_purity_real_show]}

货号：A349742 同义名： BR-A-657; Kanarb

Fimasartan 是一种改良非肽类血管紧张素 II 受体拮抗剂，常用于高血压与心力衰竭的研究。

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Fimasartan/非马沙坦 化学结构 CAS号：247257-48-3
Fimasartan/非马沙坦 化学结构
CAS号：247257-48-3
Fimasartan/非马沙坦 3D分子结构
CAS号：247257-48-3
Fimasartan/非马沙坦 化学结构 CAS号：247257-48-3
Fimasartan/非马沙坦 3D分子结构 CAS号：247257-48-3
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Fimasartan/非马沙坦 纯度/质量文件 产品仅供科研

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Fimasartan/非马沙坦 生物活性

描述 Fimasartan (BR-A-657) is an angiotensin receptor II antagonist. Fimasartan displaced angiotensin II (Ang II) from its specific binding sites to AT1 subtype receptors in membrane fractions of HEK-293 cells with an IC50 of 0.16 nM. In conscious rats, Fimasartan (0.01, 0.1, 1 mg/kg; intravenously) dose-dependently antagonized Ang II-induced pressor responses. Fimasartan dose-dependently decreased mean arterial pressure in furosemide-treated rats and renal hypertensive rats. Fimasartan given orally at 1 and 3 mg/kg reduced blood pressure in conscious renal hypertensive rats[2]. In addition, fimasartan down-regulates the expression of the iNOS (inducible nitric oxide synthase) in macrophages via NF-κB (nuclear factor-kappa B) and AP-1 (activator protein-1) inactivation[3].

Fimasartan/非马沙坦 细胞实验

Cell Line
Concentration Treated Time Description References
CD3+T cells 1 mM 5 days Evaluate the effect of Fimasartan on T cell proliferation Mol Med. 2019 Jul 15;25(1):33
LN229 cells 100μM 48 hours To evaluate the effect of Fimasartan on the viability of LN229 cells, results showed Fimasartan reduced the viability of LN229 cells Cancer Cell Int. 2023 Jun 9;23(1):111
BV2 microglia cells 30 ng/mL 6 hours To evaluate the effect of Fimasartan on NLRP3 inflammasome activation in microglia stimulated by hemolysate. Results showed that Fimasartan pretreatment significantly reduced the expression of NLRP3, ASC, and cleaved caspase-1. Exp Neurol. 2018 Dec;310:22-32
human liver microsomes 30 µM 10 minutes To evaluate the effect of POH on FMS metabolism, it was found that POH increased the formation of BR-A-557 but decreased the formation of FMS S-oxide. Pharmaceutics. 2024 Dec 11;16(12):1581
3T3-L1 cells 0.14 mmole 24 hours Fimasartan decreased lipid contents in differentiated 3T3-L1 cells. PPAR Res. 2017;2017:8048720
HepG2 cells 0.14 mmole 24 hours Fimasartan increased the protein levels of PPARδ, p-AMPK, p-ACC, MCD, MCAD, and PGC-1α, and decreased the expression levels of FAS, 11β-HSDH1, and TNF-α. PPAR Res. 2017;2017:8048720
HK-2 cells 62.5 and 125 µM 24 hours To evaluate the effects of Fimasartan on ATII expression, MAPKs phosphorylation, Nrf2 pathway, and antioxidant enzyme expression in TNF-α-stimulated HK-2 cells. Results showed that Fimasartan inhibited ATII expression, reduced phosphorylation of JNK and ERK1/2, increased nuclear Nrf2 expression, and upregulated downstream antioxidant enzymes (e.g., NQO1 and HO-1). Int J Med Sci. 2015 Oct 21;12(11):891-904

Fimasartan/非马沙坦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
ApoE KO mice Carotid artery injury model Oral gavage 3 mg/kg/day Once daily for 28 days Evaluate the effect of Fimasartan on neointimal formation and inflammation after carotid artery injury Mol Med. 2019 Jul 15;25(1):33
Sprague-Dawley rats Collagenase-induced intracerebral hemorrhage model Oral 0.5, 1.0, and 3.0 mg/kg Once daily for 30 days pretreatment and continued for 3 days post-surgery To evaluate the effect of Fimasartan pretreatment on brain injury and neuroinflammation after intracerebral hemorrhage. Results showed that low-dose Fimasartan (0.5 mg/kg) significantly attenuated brain edema, improved neurological functions, and inhibited the activation of NLRP3 inflammasome and NF-κB pathway without significantly lowering blood pressure. Exp Neurol. 2018 Dec;310:22-32
Sprague-Dawley rats Hypertension model Gastrointestinal injection 0.5 mg/kg Single dose To evaluate the regional absorption of Fimasartan in different gastrointestinal segments, showing the highest absorption in the small intestine (49.7%±11.5%), followed by duodenum (23.0%±12.1%), large intestine (19.1%±11.9%), and stomach (8.2%±3.2%) Pharmaceutics. 2018 Oct 3;10(4):174
Spontaneously hypertensive rats (SHRs) High-fat diet-induced NAFLD model Oral 10 mg/kg/day Once daily for 8 weeks Fimasartan increased the protein levels of PPARδ, p-AMPK, and PGC-1α in liver tissues, elevated SDH activity and ATP concentration, and reduced triglyceride levels in the liver. Additionally, it increased adiponectin levels in visceral fat tissues. PPAR Res. 2017;2017:8048720
Healthy male volunteers Healthy humans Oral 60 mg Single dose To investigate the influence of high sodium diet on the pharmacokinetics and pharmacodynamics of fimasartan. Results showed no significant effect of high sodium diet on the systemic exposure of fimasartan. Drug Des Devel Ther. 2016 Apr 19;10:1525-31
C57BL/6 mice Unilateral ureteral obstruction (UUO) model Intraperitoneal injection 3 mg/kg/day Once daily for 7 days To evaluate the effects of Fimasartan on UUO-induced renal inflammation, fibrosis, oxidative stress, and Nrf2 pathway. Results showed that Fimasartan significantly attenuated renal fibrosis, reduced inflammatory cell infiltration, inhibited RAS activation and Nox expression, upregulated Nrf2 and its downstream antioxidant enzymes, and decreased renal apoptosis. Int J Med Sci. 2015 Oct 21;12(11):891-904
Sprague-Dawley rats Myocardial infarction model Oral 10 mg/kg/day Once daily for 7 weeks To evaluate the effect of fimasartan on cardiac remodeling after MI. Results showed that the fimasartan-treated group had a higher mean ejection fraction and smaller left ventricular end-diastolic diameter compared to the MI-only group, and the infarct size was also smaller. J Clin Med. 2019 Mar 15;8(3):366

Fimasartan/非马沙坦 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
NCT03649646 - Recruiting September 9, 2020 Korea, Republic of ... 展开 >> Ajou University Hospital Recruiting Suwon, Korea, Republic of Contact: Seung-Jae Tahk 收起 <<
NCT02394392 - Completed - Korea, Republic of ... 展开 >> Korea university Guro hospital Seoul, Korea, Republic of 收起 <<
NCT03254914 - Recruiting September 30, 2019 Korea, Republic of ... 展开 >> Seoul national university hospital Recruiting Seoul, Korea, Republic of Contact: Hae-young Lee, MD 收起 <<

Fimasartan/非马沙坦 参考文献

[1]Ryu S, et al. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol Pharm Bull. 2013;36(3):467-74.

[2]Chi YH, Lee JH, Kim JH, Tan HK, Kim SL, Lee JY, Rim HK, Paik SH, Lee KT. Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist. Biol Pharm Bull. 2013;36(7):1208-15.

[3]Ryu S, Shin JS, Cho YW, Kim HK, Paik SH, Lee JH, Chi YH, Kim JH, Kim JH, Lee KT. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol Pharm Bull. 2013;36(3):467-74.

Fimasartan/非马沙坦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.93mL

3.99mL

1.99mL

Fimasartan/非马沙坦 技术信息

CAS号247257-48-3
分子式C27H31N7OS
分子量 501.65
SMILES Code S=C(N(C)C)CC1=C(C)N=C(CCCC)N(CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)C1=O
MDL No. MFCD13194795
别名 BR-A-657; Kanarb
运输蓝冰
InChI Key AMEROGPZOLAFBN-UHFFFAOYSA-N
Pubchem ID 9870652
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 50 mg/mL(99.67 mM)，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

Tags: Fimasartan | 247257-48-3 | BR-A-657 | Angiotensin Receptor | 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 | Fimasartan/非马沙坦 纯度/质量文件 | Fimasartan/非马沙坦 生物活性 | Fimasartan/非马沙坦 临床数据 | Fimasartan/非马沙坦 参考文献 | Fimasartan/非马沙坦 实验方案 | Fimasartan/非马沙坦 技术信息

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