1. GPCR/G Protein Apoptosis
  2. Angiotensin Receptor Apoptosis
  3. Fimasartan

Fimasartan  (Synonyms: 非马沙坦; BR-A-657)

目录号: HY-B0780 纯度: 98.55%
COA 产品使用指南

Fimasartan(BR-A-657) 是血管紧张素受体 AT1 非肽类拮抗剂,用于研究高血压和心力衰竭。

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Fimasartan Chemical Structure

Fimasartan Chemical Structure

CAS No. : 247257-48-3

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10 mM * 1 mL in DMSO ¥1048
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5 mg ¥300
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10 mg ¥500
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50 mg ¥1100
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Other Forms of Fimasartan:

查看 Angiotensin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure. IC50 value: Target: AT1 receptor antagonist in vitro: Fimasartan suppressed the expressions of inducible nitric oxide synthase (iNOS) by down-regulating its transcription, and subsequently inhibited the productions of nitric oxide (NO). In addition, fimasartan attenuated LPS-induced transcriptional and DNA-binding activities of nuclear factor-kappa B (NF-κB) and activator protein-1 (AP-1) [1]. BR-A-657 displaced [125I][Sar1 -Ile8]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 [2]. in vivo: After oral administration of 240 mg fimasartan, the mean area under the plasma concentration-time curve from time zero to infinity was 2899.0 ng/ml/h in the older, which was significantly greater than in young subjects (1767.4 ng/ml/h; p = 0.03) [3]. Compared with atorvastatin alone, coadministration of fimasartan and atorvastatin increased the atorvastatin acid mean (95% confidence interval) maximum concentration (Cmax,ss) by 1.89-fold (1.49-2.39) and the area under the concentration curve (AUCτ,ss) by 1.19-fold (0.96-1.48). Fimasartan also increased the mean 2-hydroxy atorvastatin acid Cmax,ss and AUCτ,ss by 2.45-fold (1.80-3.35) and 1.42-fold (1.09-1.85), respectively [4].

IC50 & Target

AT1 Receptor

 

Clinical Trial
分子量

501.65

Formula

C27H31N7OS

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

非马沙坦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 49 mg/mL (97.68 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9934 mL 9.9671 mL 19.9342 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9934 mL 9.9671 mL 19.9342 mL 49.8355 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL 9.9671 mL
10 mM 0.1993 mL 0.9967 mL 1.9934 mL 4.9836 mL
15 mM 0.1329 mL 0.6645 mL 1.3289 mL 3.3224 mL
20 mM 0.0997 mL 0.4984 mL 0.9967 mL 2.4918 mL
25 mM 0.0797 mL 0.3987 mL 0.7974 mL 1.9934 mL
30 mM 0.0664 mL 0.3322 mL 0.6645 mL 1.6612 mL
40 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2459 mL
50 mM 0.0399 mL 0.1993 mL 0.3987 mL 0.9967 mL
60 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8306 mL
80 mM 0.0249 mL 0.1246 mL 0.2492 mL 0.6229 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Fimasartan
目录号:
HY-B0780
需求量: