呱氨托美丁

呱氨托美丁用途

氨甲喋呤-瓜氨酸是一种有效的非甾体抗炎药,具有镇痛作用。Amtolmetin guacil抑制前列腺素合成和环氧合酶(COX)。Amtolmetin guacil可以刺激胃肠道壁上的辣椒素受体,并释放胃保护性一氧化氮(NO)。Amtolmetin guacil可用于研究膝关节骨关节炎[1][2]。

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呱氨托美丁名称

[ CAS 号 ]:
87344-06-7

[ 中文名 ]:
哌氨托美丁

[ 英文名 ]:
Amtolmetin guacil

[中文别名 ]:

呱氨托美丁

[英文别名 ]:

amtolmetin guacil
MFCD00866153

呱氨托美丁生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 一氧化氮合酶

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

Prostaglandin receptor, COX, NO[1][2]

[体外研究]

在大鼠新鲜血浆和大鼠肝微粒体中,氨甲酰胍(100μM；0-60分钟)与MED5(1-甲基-5-对甲基苯甲酰基-吡咯-2-乙酰氨基乙酸)一起转化为TMT(托尔梅汀,HY-B1799),快速转化为MED5和MED5甲酯,而在人新鲜血浆和人肝微粒体内不产生TMT[3]。

[体内研究]

动物模型：雄性Wistar大鼠[3]剂量：50 mg/kg给药：p.o。；单剂量结果：Amtolmetin guacil在雄性Wistar大鼠体内的药代动力学参数[3]。AUC0-t(ng/mL·h)AUC0-∞ (ng/mL·h)Cmax(μg/mL)Tmax(h)Kel(h-1)t1/2,β

呱氨托美丁物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
663.3±55.0 °C at 760 mmHg

[ 熔点 ]:
117-120ºC

[ 分子式 ]:
C₂₄H₂₄N₂O₅

[ 分子量 ]:
420.458

[ 闪点 ]:
354.9±31.5 °C

[ 精确质量 ]:
420.168518

[ PSA ]:
86.63000

[ LogP ]:
1.98

[ 外观性状 ]:
白色针状晶体

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
室温，干燥

呱氨托美丁MSDS

详细MSDS(安全技术说明书)

呱氨托美丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MC0598400

CHEMICAL NAME :: Glycine, N-((1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl)acety l)-, 2-methoxyphenyl ester

CAS REGISTRY NUMBER :: 87344-06-7

LAST UPDATED :: 199512

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C24-H24-N2-O5

MOLECULAR WEIGHT :: 420.50

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1450 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1370 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417