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Merck
CN

T0318

Sigma-Aldrich

曲尼司特

≥98% (HPLC), powder

别名:

2-[[3-(3,4-二甲氧基苯基)-1-氧代-2-丙烯基] 氨基] 苯甲酸, 3,4-DAA, N-(3,4-二甲氧基肉桂酰)邻氨基苯甲酸, SB-252218, 利喘平

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About This Item

经验公式(希尔记法):
C18H17NO5
CAS号:
分子量:
327.33
MDL编号:
UNSPSC代码:
41106500
PubChem化学物质编号:
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

mp

166.2-168.2 °C (lit.)

溶解性

DMSO: >10 mg/mL
H2O: insoluble

创始人

Kissei

储存温度

2-8°C

SMILES字符串

COc1ccc(\C=C\C(=O)Nc2ccccc2C(O)=O)cc1OC

InChI

1S/C18H17NO5/c1-23-15-9-7-12(11-16(15)24-2)8-10-17(20)19-14-6-4-3-5-13(14)18(21)22/h3-11H,1-2H3,(H,19,20)(H,21,22)/b10-8+

InChI key

NZHGWWWHIYHZNX-CSKARUKUSA-N

基因信息

应用

在小鼠骨髓来源的肥大细胞中研究了曲尼司特对肥大细胞表面受体的作用。

生化/生理作用

曲尼司特是一种抗哮喘药物,可抑制刺激单核细胞 LTC 4 和 PGE 2 的形成,但不抑制环氧合酶或脂氧合酶活性;抑制肥大细胞脱颗粒;在体内抑制 VEGF 诱导的血管生成 ,在体外也抑制人内皮细胞的增殖和管道形成 。曲尼司特可能代表一类新的治疗 T H 1 介导的自身免疫性疾病的药物。
曲尼司特还通过抑制细胞周期蛋白依赖性激酶抑制剂-1(p21Waf1 / Cip1)来抑制血管平滑肌细胞的增殖,它可用于治疗心脏同种异体移植物血管病变(cardiac allograft vasculopathy)。它用于治疗肥厚性瘢痕和瘢痕疙瘩。曲尼司特会抑制肿瘤坏死因子(TNF-α和TGF-β2),从而阻碍人视网膜色素上皮细胞系(ARPE)的上皮间质转化。

特点和优势

该化合物由 Kissei 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

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral

储存分类代码

11 - Combustible Solids

WGK

WGK 3

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


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Philippe Lachapelle et al.
Pharmacology & therapeutics, 187, 98-113 (2018-02-21)
The transforming growth factor (TGF)-β cytokines play a central role in development and progression of chronic respiratory diseases. TGF-β overexpression in chronic inflammation, remodeling, fibrotic process and susceptibility to viral infection is established in the most prevalent chronic respiratory diseases
Tranilast inhibits cardiac allograft vasculopathy in association with p21waf1/cip1 expression on neointimal cells in murine cardiac transplantation model
Izawa A, et al.
Arteriosclerosis, Thrombosis, and Vascular Biology, 21(7), 1172-1178 (2001)
Henrik Brovold et al.
Scientific reports, 9(1), 10513-10513 (2019-07-22)
Several epidemiological studies have pointed at serum uric acid (SUA) as an independent risk factor for mortality, diabetes, hypertension, cardiovascular and kidney disease; however, no clear pathogenic pathway is established. Uric acid (UA) crystals show pro-inflammatory properties and can thus
Kaname Uno et al.
Journal of clinical gastroenterology, 46(9), e76-e82 (2012-09-08)
As circumferential or near-circumferential endoscopic submucosal dissection (ESD) for superficial esophageal neoplasms might evoke refractory strictures, multiple sessions of endoscopic balloon dilation (EBD) are required. We aimed to assess the effectiveness and safety of oral agent tranilast with EBD for
Natsuko Kageyama-Yahara et al.
FEBS letters, 584(1), 111-118 (2009-11-12)
Mast cell activation by immunoglobulin E (IgE)-mediated stimuli is a central event in the pathogenesis of allergic disorders. The present report shows that treatment with pentagalloylglucose (PGG) resulted in a down-regulation of FcepsilonRI surface expression on mucosal-type murine bone marrow-derived

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