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曲尼司特

抗炎药
规格或纯度: ≥98% (HPLC)
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货号 (SKU) 包装规格 是否现货 价格 数量
T129491-250mg 250mg 现货 Stock Image
T129491-1g 1g 现货 Stock Image
T129491-5g 5g 现货 Stock Image
T129491-25g 25g 现货 Stock Image
T129491-100g 100g 现货 Stock Image
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药物成分

基本描述

规格或纯度 ≥98% (HPLC)
英文名称 Tranilast
别名 曲尼司特;N-(3,4-二甲氧基肉桂酰)邻氨基苯甲酸;2-[[3-(3,4-二甲氧基苯基)-1-氧代-2-丙烯基] 氨基] 苯甲酸;SB-252218;利喘平;2-[[3-(3,4-二甲氧基苯基)-1-氧-2-丙烯基]氨基]苯甲酸;N-(3,4-二甲氧基肉桂酰)氨茴酸;曲尼斯特
英文别名 MK-341;N-(3,4-Dimethoxycinnamoyl)anthranilic Acid;2-[[3-(3,4-Dimethoxyphenyl)-1-oxo-2-propenyl]amino]benzoic Acid;MK 341; Rizaben; Tranpro; SB 252218 ;3,4-DAA;2-[[(E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]benzoic acid
生化机理 Tranilast is an angiogenesis inhibitor that also inhibits the release of histamine and prostaglandins from basophils and mast cells. Other functions of Tranilast include the ability to inhibit leukotrienes, oxygen radicals, cyclooxygenase-2 expression, cytokines, collagen synthesis, and blocks the production of IL-1 and IL-2 from human T-cells and macrophages. Studies indicate that Tranilast blocks vascular inflammation and disrupts the NF-κB/CBP interaction, which leads to the inhibition of NF-κB dependent transcription activation. Additionally, Tranilast has been reported to inhibit the release of PGE2 and TGF-β from monocytes-macrophages and the transformation of fibroblasts to myofibroblasts, and contraction in vitro. Smooth muscle cell studies have revealed that Tranilast inhibits vascular smooth muscle cell growth, calcium entry, and acts as an antagonist of Angiotensin (angiotensin II).Potent mast cell membrane stabilizer. Exhibits a wide range of anti-inflammatory effects. Inhibits antigen-induced release of cytokines, chemokines and proteases. Able to inhibit angiotensin II induced contractions (IC 50 = 36 μM).
应用 An inhibitor of angiogenesis and the release of histamine and prostaglandins.
储存温度 2-8°C储存
运输条件 冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Tranilast is an antiallergic drμg by inhibiting lipid mediator and cytokine release from inflammatory cells, used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.An inhibitor of angiogenesis and the release of histamine and prostaglandins.

Tranilast is an antiallergic drug by inhibiting lipid mediator and cytokine release from inflammatory cells, used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.
An inhibitor of angiogenesis and the release of histamine and prostaglandins.

名称和标识符

IUPAC Name 2-[[(E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]benzoic acid
INCHI 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
Canonical SMILES COC1=C(C=C(C=C1)C=CC(=O)NC2=CC=CC=C2C(=O)O)OC
分子式

C18H17NO5

关联CAS 70806-55-2
PubChem CID 5282230
分子量 327.33

化学和物理性质

溶解性 Soluble in DMSO (>10 mg/ml), water (<1 mg/ml), and ethanol (<1 mg/ml).
敏感性 对热敏感
熔点 166.2-168.2 °C

安全信息

象形图
ghs07

Harmful

信号词 Warning
危险声明 H302: Harmful if swallowed
预防措施声明 P501,P264,P270,P330,P301+P317
WGK Germany 3
RTECS DG8731000
Merck Index 9570
个人防护装备 dust mask type N95 (US), Eyeshields, Gloves

参考文献

1. Quayle LA et al..  (2017)  Anti-angiogenic drugs: direct anti-cancer agents with mitochondrial mechanisms of action..  Oncotarget,  (51):  (88670-88688).  [PMID:29179466]

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