Candesartan Cilexetil (Synonyms: 坎地沙坦酯; TCV-116)

目录号: HY-17505 纯度: 99.86%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Candesartan Cilexetil (TCV-116) 是一种血管紧张素 II 受体 (angiotensin II receptor) 抑制剂，Candesartan Cilexetil 具有改善肺纤维化，抗病毒和皮肤创面愈合作用，可用于高血压的研究。

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Candesartan Cilexetil Chemical Structure

CAS No. : 145040-37-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥605	In-stock
500 mg	￥550	In-stock
1 g	￥850	In-stock
5 g		询价
10 g		询价

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生物活性
纯度 & 产品资料
参考文献

生物活性

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor inhibitor. Candesartan Cilexetil ameliorates the pulmonary fibrosis and has antiviral and skin wound healing effect. Candesartan Cilexetil can be used for the research of high blood pressure^[1]^[2]^[3]^[4]^[5]^[6].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
16HBE14o-	IC₅₀	> 100 μM Compound: 1; CDC, MT04D0301	Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay	[PMID: 31732254]
A-431	IC₅₀	2.6 μM Compound: Candesartan cilexetil	Inhibition of IDO in human A431 cells assessed as kynurenine production after 24 hrs Inhibition of IDO in human A431 cells assessed as kynurenine production after 24 hrs	10.1039/C2MD00278G
A549	IC₅₀	63.93 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human A549 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
A549	IC₅₀	65.92 μM Compound: 1; CDC	Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay	[PMID: 33129593]
BEAS-2B	IC₅₀	79.76 μM Compound: 1; CDC	Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay	[PMID: 33129593]
BEAS-2B	IC₅₀	89.94 μM Compound: 1; CDC, MT04D0301	Cytotoxicity against human BEAS2B cells after 48 hrs by CCK-8 assay Cytotoxicity against human BEAS2B cells after 48 hrs by CCK-8 assay	[PMID: 31732254]
EKVX	IC₅₀	> 100 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
HepG2	IC₅₀	> 100 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
Huh-7	IC₅₀	> 100 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
MCF7	IC₅₀	> 100 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
MGC-803	IC₅₀	57.14 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
MKN-45	IC₅₀	68.87 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
NCI-H1299	IC₅₀	45.02 μM Compound: 1; CDC	Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay	[PMID: 33129593]
NCI-H1299	IC₅₀	45.11 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
PLC	IC₅₀	60.21 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
T47D	IC₅₀	64.35 μM Compound: 1; CDC, MT04D0301	Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]

体外研究
(In Vitro)

Candesartan Cilexetil (0.1-10 μM, 24 h) 在 HUVEC 细胞、HEK293T 细胞中均表现出对 ZIKV 的抗病毒作用^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	HUVEC cells, HEK293T cells
Concentration:	0.1 μM, 1 μM, 5 μM, 10 μM
Incubation Time:	24 h
Result:	Showed a dose-dependent antiviral effect in ZIKV-infected HUVEC and HEK293T cells.

体内研究
(In Vivo)

Candesartan Cilexetil (5 mg/kg，灌胃，一天一次，连续 7 周) 可改善高盐喂养的 Dahl 盐敏感 (DS) 大鼠的心肌重构和心力衰竭^[2]。
Candesartan Cilexetil (1-10 mg/kg，口服，一天一次，连续15 天) 对大鼠皮肤创面愈合有促进作用^[3]。
Candesartan Cilexetil (1-10 mg/kg，胃管给药，一天一次，持续 4-12 周) 可抑制自发性高血压大鼠的血压升高^[5]。
Candesartan Cilexetil (10 mg/kg，口服，饮水中补充，持续2-23 天) 可抑制 bleomycin (HY-108345) 诱导的大鼠肺纤维化模型中 TGF-b1 的合成，改善肺纤维化^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Dahl salt-sensitive hypertensive rats^[2]
Dosage:	5 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Increased body weight and decreased left ventricular end-diastolic diameter. Decreased the level of iNOS mRNA and ADM mRNA in the left ventricle (LV). Increased the eNOS protein mass in the LV and decreased the immunoreactive ADM contents of LV. Enhanced immunoreactivity for eNOS. Significantly decreased the degree of perivascular fibrosis.

Animal Model:	Skin wound model rat ^[3]
Dosage:	1 mg/kg, 10 mg/kg
Administration:	Oral
Result:	Showed 100% re-epithelization of the wound at 1 mg/kg. Significantly suppressed angiogenesis at 10 mg/kg.

Clinical Trial

分子量

610.66

Formula

C₃₃H₃₄N₆O₆

CAS 号

145040-37-5

性状

固体

颜色

White to off-white

中文名称

坎地沙坦酯

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

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (81.88 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	1.6376 mL	8.1879 mL	16.3757 mL
5 mM	0.3275 mL	1.6376 mL	3.2751 mL
10 mM	0.1638 mL	0.8188 mL	1.6376 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.09 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.09 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.86%

选择批次：

Data Sheet (648 KB) SDS (562 KB)

COA (302 KB) LCMS (92 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Loe M W C, et al. Antiviral activity of the FDA-approved drug candesartan cilexetil against Zika virus infection [J]. Antiviral Research, 2019, 172: 104637. [Content Brief]

[2]. Kobayashi N, et al. Effects of TCV-116 on expression of NOS and adrenomedullin in failing heart of Dahl salt-sensitive rats [J]. Atherosclerosis, 2001, 156(2): 255-265. [Content Brief]

[3]. Takeda H, et al. Effects of angiotensin II receptor signaling during skin wound healing [J]. The American journal of pathology, 2004, 165(5): 1653-1662. [Content Brief]

[4]. McClellan K J, et al. Candesartan cilexetil: a review of its use in essential hypertension [J]. Drugs, 1998, 56: 847-869. [Content Brief]

[5]. Kojima M, et al. Angiotensin II receptor antagonist TCV-116 induces regression of hypertensive left ventricular hypertrophy in vivo and inhibits the intracellular signaling pathway of stretch-mediated cardiomyocyte hypertrophy in vitro [J]. Circulation, 1994, 89(5): 2204-2211. [Content Brief]

[6]. Otsuka M, et al. Reduction of bleomycin induced lung fibrosis by candesartan cilexetil, an angiotensin II type 1 receptor antagonist [J]. Thorax, 2004, 59(1): 31-38. [Content Brief]

Candesartan Cilexetil 相关分类

Endocrinology Cardiovascular Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6376 mL	8.1879 mL	16.3757 mL	40.9393 mL
	5 mM	0.3275 mL	1.6376 mL	3.2751 mL	8.1879 mL
	10 mM	0.1638 mL	0.8188 mL	1.6376 mL	4.0939 mL
	15 mM	0.1092 mL	0.5459 mL	1.0917 mL	2.7293 mL
	20 mM	0.0819 mL	0.4094 mL	0.8188 mL	2.0470 mL
	25 mM	0.0655 mL	0.3275 mL	0.6550 mL	1.6376 mL
	30 mM	0.0546 mL	0.2729 mL	0.5459 mL	1.3646 mL
	40 mM	0.0409 mL	0.2047 mL	0.4094 mL	1.0235 mL
	50 mM	0.0328 mL	0.1638 mL	0.3275 mL	0.8188 mL
	60 mM	0.0273 mL	0.1365 mL	0.2729 mL	0.6823 mL
	80 mM	0.0205 mL	0.1023 mL	0.2047 mL	0.5117 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.

Keywords:

Candesartan Cilexetil145040-37-5TCV-116坎地沙坦酯TCV116TCV 116Angiotensin ReceptorApoptosisHUVEC cellsHEK293T cellsDahl salt-sensitiveSkin woundhigh blood pressureInhibitorinhibitorinhibit

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Candesartan Cilexetil (Synonyms: 坎地沙坦酯; TCV-116)

Customer Review

Other Forms of Candesartan Cilexetil:

Candesartan Cilexetil 相关抗体

MCE 顾客使用本产品发表的 2 篇科研文献

Candesartan Cilexetil 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

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

Candesartan Cilexetil 相关抗体:

摩尔计算器

稀释计算器

Candesartan Cilexetil 相关分类

完整储备液配制表

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