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Merck
CN

T8949

替米沙坦

≥98% (HPLC), AT1 angiotensin receptor antagonist, solid

别名:

4′[(1,4′-二甲基-2′-丙基 [2,6′-双-1H-苯并咪唑 ]-1′-基)甲基 ] [1,1′-联苯基 ]-2-羧酸, BIBR 277

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关于此项目

经验公式(希尔记法):
C33H30N4O2
化学文摘社编号:
分子量:
514.62
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
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产品名称

替米沙坦, ≥98% (HPLC), solid

SMILES string

CCCc1nc2c(C)cc(cc2n1Cc3ccc(cc3)-c4ccccc4C(O)=O)-c5nc6ccccc6n5C

InChI key

RMMXLENWKUUMAY-UHFFFAOYSA-N

InChI

1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)

assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: >5 mg/mL at 60 °C
H2O: insoluble

originator

Boehringer Ingelheim

Quality Level

Gene Information

human ... AGTR1(185)

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Preparation Note

替米沙坦可溶于 DMSO,浓度大于 5 mg/mL。不溶于水。

Application

替米沙坦已作为 AT1 受体拮抗剂用于研究其对心肌梗死小鼠模型的影响。本研究报道替米沙坦可抑制 CCN1 上调,降低 CCN2 水平心房心肌细胞 。替米沙坦也被用于评价其对心肌梗死小鼠肾皮质 CCN1 表达的影响 。此外,已在结直肠癌小鼠模型中测试替米沙坦检测其抑制肿瘤生长的疗效

Biochem/physiol Actions

替米沙坦是一种非肽类 1 血管紧张素受体拮抗剂。

Features and Benefits

在《受体分类和信号转导》手册的 血管紧张素受体页有该化合物的介绍。想要浏览手册的其他页面, 请单击此处
该化合物由 Boehringer Ingelheim 开发。要浏览其他制药公司开发的化合物列表批准的药物/候选药物的列表, 点击这里
这种化合物是 ADME 毒性研究的特色产品。点击此处发现更多特色 ADME 毒性产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Marc P Maillard et al.
The Journal of pharmacology and experimental therapeutics, 302(3), 1089-1095 (2002-08-17)
In vitro studies have shown that telmisartan is an insurmountable angiotensin II subtype-1 (AT1) receptor antagonist. Herein, the molecular basis of this insurmountable antagonism has been investigated in vitro, and the effect of telmisartan has been compared in vivo with
Maurizio Cortada et al.
Audiology & neuro-otology, 25(6), 297-308 (2020-05-06)
Telmisartan is an angiotensin II receptor blocker that has pleiotropic effects and protective properties in different cell types. Moreover, telmisartan has also shown partial agonism on the peroxisome proliferator-activated receptor γ (PPAR-γ). Auditory hair cells (HCs) express PPAR-γ, and the
M Sharpe et al.
Drugs, 61(10), 1501-1529 (2001-09-18)
Telmisartan is an angiotensin II receptor antagonist that is highly selective for type 1 angiotensin II receptors. It was significantly more effective than placebo in large (n >100), double-blind, randomised, multicentre clinical trials in patients with mild to moderate hypertension.
Tomasz Andrzej Bonda et al.
Folia histochemica et cytobiologica, 51(1), 84-91 (2013-05-22)
Chronic heart failure often leads to worsening of the renal function. Mediators of this process include inflammatory and neuroendocrine factors. CCN1 (Cyr 61), a member of growth factor-inducible immediate early genes, which modulates inflammation and fibrogenesis, is excreted with urine
Li Li et al.
Diabetes, 62(3), 762-774 (2012-12-15)
The mechanisms of the improvement of glucose homeostasis through angiotensin receptor blockers are not fully elucidated in hypertensive patients. We investigated the effects of telmisartan on insulin signaling and glucose uptake in cultured myotubes and skeletal muscle from wild-type and

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