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质量水平
方案
≥98% (HPLC)
表单
solid
颜色
white
溶解性
DMSO: >5 mg/mL at 60 °C
H2O: insoluble
创始人
Boehringer Ingelheim
SMILES字符串
CCCc1nc2c(C)cc(cc2n1Cc3ccc(cc3)-c4ccccc4C(O)=O)-c5nc6ccccc6n5C
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)
InChI key
RMMXLENWKUUMAY-UHFFFAOYSA-N
基因信息
human ... AGTR1(185)
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应用
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 。
生化/生理作用
替米沙坦是一种非肽类 1 血管紧张素受体拮抗剂。
特点和优势
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。
制备说明
替米沙坦可溶于 DMSO，浓度大于 5 mg/mL。不溶于水。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
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
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.
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
Eleanor I Ager et al.
BMC cancer, 11, 274-274 (2011-06-28)
Targeting of the renin angiotensin system (RAS) reduces tumour growth in experimental models of cancer. We aimed to establish if combined targeting of the 'classical' and 'alternative' arms of the RAS could result in synergistic inhibition of colorectal cancer (CRC)
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