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萘丁美酮

萘丁美酮用途

Nabumetone 是一种可口服的非酸类抗炎剂,为有效的、选择性的 COX-2 抑制剂,同时是活性代谢物 6MNA 的前体物质。

萘丁美酮名称

[ CAS 号 ]:
42924-53-8

[ 中文名 ]:
萘丁美酮

[ 英文名 ]:
Nabumetone

[中文别名 ]:

[英文别名 ]:

4-(6-méthoxynaphtalén-2-yl)butan-2-one
Mebutan
Relifen
4-(6-Methoxy-2-naphthyl)-butan-2-one
Arthaxan
Relif
4-(6-Methoxynaphthalen-2-yl)butan-2-on
4-(6-methoxynaphthalen-2-yl)butan-2-one
Nabumetona
4-(6-Methoxy-2-naphthyl)butan-2-one

萘丁美酮生物活性

[ 描述 ]:

Nabumetone 是一种可口服的非酸类抗炎剂,为有效的、选择性的 COX-2 抑制剂,同时是活性代谢物 6MNA 的前体物质。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

[ 靶点 ]

COX-2

[体外研究]

Nabumetone是一种有效的选择性COX-2抑制剂。萘丁酮(50μmol-2 mmol)剂量依赖性地抑制K-562和Meg-01细胞的增殖,但没有明显的凋亡作用。 Nabumetone增强了K-562细胞系中ADR的凋亡作用。此外,Nabumetone降低Bcl-2的表达[1]。

[体内研究]

Nabumetone(79mg/kg,po)抑制大鼠的爪水肿和爪子渗出物PGE2。 Nabumetone不会诱导胃损伤,并且仅对大鼠胃粘膜6-keto-PGF1α的产生有57％的抑制作用[2]。萘丁酮(25,50,100mg/kg,ip)剂量依赖性地抑制DDC诱导的粘液分泌的增加并刺激大鼠中应激诱导的粘液分泌。 Nabumetone(25 mg/kg,ip)可显着抑制大鼠应激性溃疡指数[3]。

[细胞实验]

将每种细胞系以3×105 / mL的浓度接种到6孔板中，使用或不使用药物（Nabumetone等），并孵育48小时。然后使用台盼蓝染料排除测试计数活细胞。增殖抑制的百分比计算为1-（暴露于对照中的药物/活细胞的活细胞）×100 [1]。

[动物实验]

在研究中使用大鼠[3]白化雄性大鼠（体重250-300g）。将动物保持在单个笼中，并在实验开始前将其丢弃16小时。在实验开始前1小时允许自由饮水。每组有8只大鼠。用25-，50-或100-mg / kg剂量腹膜内注射Nabumetone或安乃近预处理动物3天[3]。

[参考文献]

[1]. Vural F, et al. Cyclo-oxygenase 2 inhibitor, nabumetone, inhibits proliferation in chronic myeloid leukemia cell lines. Leuk Lymphoma. 2005 May;46(5):753-6.

[2]. Melarange R, et al. Anti-inflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6MNA (6-methoxy-2-naphthylacetic acid): comparison with indomethacin. Agents Actions. 1992;Spec No:C82-3.

[相关活性小分子]

萘丁美酮物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
371.1±17.0 °C at 760 mmHg

[ 熔点 ]:
80-81ºC

[ 分子式 ]:
C₁₅H₁₆O₂

[ 分子量 ]:
228.286

[ 闪点 ]:
165.4±14.5 °C

[ 精确质量 ]:
228.115036

[ PSA ]:
26.30000

[ LogP ]:
2.82

[ 外观性状 ]:
白色/近乎于白色,结晶粉末

[ 蒸汽压 ]:
0.0±0.8 mmHg at 25°C

[ 折射率 ]:
1.576

[ 储存条件 ]:
Refrigerator

萘丁美酮MSDS

萘丁美酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EL9085000

CHEMICAL NAME :: 2-Butanone, 4-(6-methoxy-2-naphthalenyl)-

CAS REGISTRY NUMBER :: 42924-53-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C15-H16-O2

MOLECULAR WEIGHT :: 228.31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1260 mg/kg/6W-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - fibrosis (interstitial) Lungs, Thorax, or Respiration - cough Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 67,1021,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3880 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1520 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4290 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay) Gastrointestinal - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2380 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 3200 mg/kg

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2939,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 58240 mg/kg/26W-I

TOXIC EFFECTS :: Gastrointestinal - peritonitis Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2953,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 58240 mg/kg/26W-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2953,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 81900 mg/kg/52W-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - other changes Endocrine - changes in thymus weight

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2953,1988 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1760 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2975,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8960 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2953,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4160 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,2975,1988

萘丁美酮安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-40

[ 安全声明 (欧洲) ]:
36/37

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
EL9085000

[ 海关编码 ]:
2914399090

萘丁美酮合成路线

萘丁美酮上下游产品

萘丁美酮上游产品

萘丁美酮下游产品

萘丁美酮海关

[ 海关编码 ]: 2914509090

[ 中文概述 ]:
2914509090 含其他含氧基的酮. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:5.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙酮报明包装

[ Summary ]:
HS:2914509090 other ketones with other oxygen function VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:5.5% General tariff:30.0%

萘丁美酮文献

Exploration of alternate catalytic mechanisms and optimization strategies for retroaldolase design.

J. Mol. Biol. 426(1) , 256-71, (2014)

Designed retroaldolases have utilized a nucleophilic lysine to promote carbon-carbon bond cleavage of β-hydroxy-ketones via a covalent Schiff base intermediate. Previous computational designs have inc...

Hypersensitivity to nabumetone: cross reactivity with naproxen.

Ann. Allergy Asthma Immunol. 111(1) , 74-5, (2013)

Effects of nabumetone and dipyrone on experimentally induced gastric ulcers in rats.

Inflammation 36(2) , 476-81, (2013)

Nabumetone and dipyrone are non-acidic, nonsteroidal anti-inflammatory drugs. Both of them are known to have weak inhibitory effects of cyclooxygenases. Gastric side effects represent the most common ...

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