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K1136

Sigma-Aldrich

酮咯酸 三羟甲基氨基甲烷盐

≥99%, crystalline

别名:

托拉多尔, （±）-5-苄基-2,3-二氢-1H-吡咯嗪-1羧酸 三羟甲基氨基甲烷盐

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About This Item

经验公式（希尔记法）:
C15H13NO3 · C4H11NO3
CAS号:
74103-07-4
分子量:
376.40
MDL编号:
MFCD00887595
UNSPSC代码:
12352202
PubChem化学物质编号:
24278503
NACRES:
NA.77

生物来源

synthetic (organic)

质量水平

100

方案

≥99%

表单

crystalline

溶解性

H2O: soluble 15 mg/mL, clear, colorless to faintly yellow (stable at least one month at −20 °C.)

储存温度

room temp

SMILES字符串

NC(CO)(CO)CO.OC(=O)C1CCn2c1ccc2C(=O)c3ccccc3

InChI

1S/C15H13NO3.C4H11NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13;5-4(1-6,2-7)3-8/h1-7,11H,8-9H2,(H,18,19);6-8H,1-3,5H2

InChI key

BWHLPLXXIDYSNW-UHFFFAOYSA-N

基因信息

human ... PTGS1(5742) , PTGS2(5743)

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应用

酮咯酸已被用于：
  • 小鼠腹膜内注射，用于研究酮咯酸对ARC（下丘脑弓状核）POMC（促黑素皮质激素）-EGFP（增强型绿色荧光蛋白）神经元中c-Fos（人类原癌基因）表达的影响。
  • 对小鼠进行治疗，以研究这种治疗方法不会阻止IL-1β介导的抑制小鼠下丘脑外植体分泌Agouti相关蛋白（AgRP）的分泌。
  • 通过将角叉菜胶注射到脚踝作为镇痛药来治疗急性炎症性关节损伤的大鼠

生化/生理作用

酮咯酸是一种非甾体类药物，具有中度消炎活性，同时也是一种强效的止痛药。在中度至重度术后疼痛患者中，它具有优于吗啡等阿片类止痛片的止痛作用。它会抑制花生四烯酸和胶原蛋白引发的前列腺素合成和血小板聚集。它是一种双重COX-1 / COX-2抑制剂。

注意

如在室温下储存，至少可稳定 2 年。

象形图

Skull and crossbones
GHS06

警示用语：

Danger

危险分类

Acute Tox. 3 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

靶器官

Respiratory system

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

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分析证书(COA)

Lot/Batch Number
MKCW9383
MKCV0186
MKCQ7512
MKCJ8295
MKCH2969

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O Laneuville et al.
The Journal of pharmacology and experimental therapeutics, 271(2), 927-934 (1994-11-01)
We developed an in vitro expression system for accurate kinetic analyses of the inhibition of the human prostaglandin H synthase isozymes (hPGHS-1 and -2) by nonsteroidal anti-inflammatory drugs (NSAIDs). Assays of instantaneous inhibition in which enzyme, 10 microM arachidonate, and
Rachel L Ruhlen et al.
The Journal of the American Osteopathic Association, 113(10), 738-752 (2013-10-03)
Animal models can be used to investigate manual therapy mechanisms, but testing manipulation in animal models is problematic because animals cannot directly report their pain. To develop a rat model of inflammatory joint injury to test the efficacy of manual
M M Buckley et al.
Drugs, 39(1), 86-109 (1990-01-01)
Ketorolac is a non-steroidal agent with potent analgesic and moderate anti-inflammatory activity. It is administered as the tromethamine salt orally, intramuscularly, intravenously, and as a topical ophthalmic solution. Clinical studies indicate single-dose efficacy greater than that of morphine, pethidine (meperidine)
R A Dionne et al.
Clinical and experimental rheumatology, 19(6 Suppl 25), S63-S70 (2001-11-07)
While non-steroidal anti-inflammatory drugs (NSAIDs) are the mainstay of therapy for the management of acute pain and rheumatoid arthritis, toxicity associated with chronic administration limits their benefit-to-risk relationship in many patients. A series of studies is reviewed that assesses the
G Cirino et al.
British journal of pharmacology, 117(7), 1421-1426 (1996-04-01)
1. The effects of novel nitric oxide-releasing nonsteroidal anti-inflammatory compounds (NO-NSAIDs) on induction of nitric oxide (NO) synthase by bacterial lipopolysaccharide (LPS) were examined in a murine cultured macrophage cell line, J774. 2. LPS-induced nitrite production was markedly attenuated by
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感应染料

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Sensor Dyes

Nitric oxide (NO) as a signal transporter in neurons, endothelial cells and in the immune system.

Chromatograms

application for HPLC

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