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Merck
CN

K1136

酮咯酸 三羟甲基氨基甲烷盐

synthetic (organic), ≥99%, COX inhibitor, 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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关于此项目

经验公式（希尔记法）:
C15H13NO3 · C4H11NO3
化学文摘社编号:
74103-07-4
分子量:
376.40
UNSPSC Code:
12352202
PubChem Substance ID:
24278503
NACRES:
NA.77
MDL number:
MFCD00887595

主要文件

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产品名称

酮咯酸 三羟甲基氨基甲烷盐, ≥99%, crystalline

SMILES string

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

biological source

synthetic (organic)

assay

≥99%

form

crystalline

solubility

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

storage temp.

room temp

Quality Level

100

Gene Information

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

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相关类别

Application

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

Biochem/physiol Actions

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。

Disclaimer

如在室温下储存，至少可稳定 2 年。

pictograms

Skull and crossbones
GHS06

signalword

Danger

Hazard Classifications

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

target_organs

Respiratory system

存储类别

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
MKCW9383
MKCV0186
MKCQ7512
MKCJ8295
MKCH2969

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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
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)
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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Sensor Dyes

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

感应染料

一氧化氮 (NO) 是神经元、内皮细胞和免疫系统中的信号转运分子。

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