Telmisattan.|144701-48-4|(替米沙坦; BIBR 277)-陌孚医药/Medlife

您当前的位置：

Telmisattan. (Synonyms: 替米沙坦; BIBR 277)

目录号: PC10446 纯度: ≥98%

CAS No. :144701-48-4

商品编号	规格	价格	会员价
PC10446-50mg	50mg	¥490.00	请登录
PC10446-100mg	100mg	¥833.00	请登录
PC10446-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥637.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称

Telmisattan.

中文别名

替米沙坦;4-{[2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)苯并咪唑-1-基]甲基}联苯基-2-羧酸;4'-[[2-丙基-4-甲基-6(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基]甲基]-2-联苯羧酸;4′-[4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-丙基-1H-苯并咪唑-1-基甲基]联苯基-2-羧酸;替米沙坦 4'-[(1,4'-二甲基-2'-丙基[2,6'-联-1氢-苯并咪唑]-1'-基)甲基]-[1,1'-联苯]-2-羧酸;4'-[[1,4'-二甲基-2'-丙基[2,6'-联-1H-苯并咪唑]-1'-甲基]-[1,1'-联苯基]-2-羧酸,二甲基乙基酯;泰米沙坦;2-(2H-苯并三唑)-5-正己氧基苯酚;4'-[[1,4'-二甲基-2'-丙基(2,6'-联-1H-苯并咪唑)-1'-甲基]-[1,1'-联苯基]-2-羧酸叔丁酯;4-[4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-丙基-1H-苯并咪唑基甲基]联苯基-2-羧酸;Telmisartan 替米沙坦;氘代丁醇;替米沙;替米沙坦 EP标准品;替米沙坦 USP标准品;替米沙坦标准品;替米沙坦峰鉴别 EP标准品;替米沙坦及其杂质标准品;替米沙坦系统适应性 EP标准品;盐酸坦索罗辛-D4;4'-[[2-丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基]甲基]-2-联苯羧酸;4'-[[4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-丙基-1H-苯并咪唑-1-基]甲基]联苯-2-羧酸

英文名称

Telmisattan

英文别名

4'-((1,7'-Dimethyl-2'-propyl-1H,3'H-[2,5'-bibenzo[d]imidazol]-3'-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid;TU-199;TELMISARTAN;PRITOR;MICARDIS;BIBR 277;4'[(1,4'-DIMETHYL-2'-PROPYL[2,6'-BI-1H-BENZIMIDAZOL]-1'-YL)METHYL][1,1'-BIPHENYL]-2-CARBOXYLIC ACID;4'-[(1,4'-DIMETHYL-2'-PROPYL[2,6'-BI-H-BENZIMIDAZOL]-1'-YL)METHYL][1,1'-BIPHENYL]-2-CARBOXYLIC ACID;3-methoxy-8-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methyl sulfinyl]-2,7,9-triazabicyclo[4.3.0]nona-2,4,8,10-tetraene;4′[(1,4′-Dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-carboxylic acid;4'-[[4-Methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl]biphenyl-2-carboxylic Acid;替米沙坦;Kinzalmono;BIBR 277SE;Telmisattan;Targit;Telmisartan [INN];4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid;U5SYW473RQ;C33H30N4O2;2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]ph

Cas No.

144701-48-4

分子式

C₃₃H₃₀N₄O₂

分子量

514.62

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of I-AngII to AT1 receptors with IC₅₀ of 9.2 nM.

性状

Solid

IC50 & Target[1][2]

IC50: 9.2 nM (angiotensin II type 1 receptor)

体外研究(In Vitro)

In intact RVSMC cells and in membrane preparations, telmisartan inhibits the binding of I-AngII to AT1 receptors in a concentration-dependent manner, with an IC₅₀ of 9.2 ± 0.8 nM. In the same experimental conditions, angiotensin II displaces I-AngII with an IC₅₀ value of 2.9 ± 0.5 nM. The specific binding of [H]telmisartan to SMC membranes is displaced by unlabeled telmisartan with an IC₅₀ of 7.7 ± 1.8 nM and by cold AngII with an IC₅₀ of 32.7 ± 5.7 nM . Telmisartan treatment (100 μM) reduces the proliferation of three EAC cell lines (OE19, OE33, and SKGT-4), induces cell cycle arrest in G0/G1 phase and regulates cell cycle-related proteins in EAC cells, and induces the phosphorylation of AMPK and regulates cell cycle-related proteins via the AMPK/mTOR pathway in EAC cells. Telmisartan inhibits the activation of RTKs, downstream effectors and cell cycle-related proteins.

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

体内研究(In Vivo)

In the telmisartan (0.1, 0.3, and 1 mg/kg)-treated rats, the specific binding of [H]telmisartan to the surface of living RVSMC is saturable and increases quickly to reach equilibrium within 1 h. Telmisartan dissociates very slowly from the receptor with a dissociation half-life (t1/2) of 75 min, which is comparable with candesartan and almost 5 times slower than angiotensin II (AngII). In vivo, telmisartan blunts the blood pressure response to exogenous AngII dose dependently. Telmisartan (10 mg/kg/d) administration effectively suppresses aneurysm pathogenesis after PPE infusion as well, regardless of whether treatment is initiated before or after aneurysm creation or continues for a limited or extended time. Telmisartan treatment is associated with reduced messenger RNA levels for CCL5 and matrix metalloproteinases 2 and 9 in aneurysmal aortae, with no apparent effect on PPARγ-regulated gene expression. Telmisartan (1 mg/kg/day) significantly ameliorates neuronal loss and the spatial acquisition impairment in 5XFAD mice, but without any changes of NeuN expression in the hippocampus layer. Telmisartan (1 mg/kg/day) treatment reduces amyloid burden and microglial accumulation in 5XFAD mice brain, induces microglial polarization towards neuroprotective phenotype, but does not alter the expression levels of NEP and IDE in 5XFAD mice specific brain areas. Telmisartan (0.05, 0.1, 1 mg/kg, p.o.) shows significant reduction in immobility time, antagonizes depression and anxiety, and also significantly attenuates serum cortisol, NO, IL-6 and IL-1β in rats. Telmisartan (50 μg, i.p.) leads to a 73.2% reduction in tumor growth in mice bearing xenografts derived from OE19 cells. Furthermore, miRNA expression is significantly altered by telmisartan in vivo.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Maillard MP, et al. 体外研究 and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1089-95. [Information]

[2]. Xuan H, et al. Inhibition or deletion of angiotensin II type 1 receptor suppresses elastase-induced experimental abdominal aortic aneurysms. J Vasc Surg. 2017 Apr 20. pii: S0741-5214(17)30100-3. [Information]

[3]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimers disease mice. Brain Behav Immun. 2017 Apr 3. [Information]

[4]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364. [Information]

[5]. Fujihara S, et al. The angiotensin II type 1 receptor antagonist telmisartan inhibits cell proliferation and tumor growth of esophageal adenocarcinoma via the AMPKα/mTOR pathway 体外研究 and in vivo. Oncotarget. 2017 Jan 31;8(5):8536-8549. [Information]

溶解度数据

体外研究:

DMSO : 6.67 mg/mL (12.96 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9432 mL	9.7159 mL	19.4318 mL
5 mM	0.3886 mL	1.9432 mL	3.8864 mL
10 mM	0.1943 mL	0.9716 mL	1.9432 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

1.

建议依照次序添加每种溶剂： 17% Polyethylene glycol 12-hydroxystearate in saline
Solubility: 3.33 mg/mL (6.47 mM); Suspended solution; Need ultrasonic and warming
2.

建议依照次序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 3 mg/mL (5.83 mM); Suspended solution; Need ultrasonic
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution

此方案可获得 ≥ 0.67 mg/mL (1.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution

此方案可获得 ≥ 0.67 mg/mL (1.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation