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莫非佐酸

莫非佐酸用途

莫非唑酸是一种非甾体抗炎药(NSAID),是一种选择性、可逆的口服活性COX-1抑制剂,IC50为1.44 nM。莫非唑酸对COX-2的抑制活性较弱(IC50为447nm)。莫非佐拉可缓解疼痛,并具有抗炎作用[1]。

莫非佐酸名称

[ CAS 号 ]:
78967-07-4

[ 中文名 ]:
莫非佐酸

[ 英文名 ]:
Mofezolac

[中文别名 ]:

莫苯唑酸

[英文别名 ]:

mofezolac
N-22

莫非佐酸生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

COX-1:1.44 nM (IC50)

COX-2:447 nM (IC50)

[体外研究]

在人富血小板血浆(hPRP)测定中,莫非佐拉抑制血小板聚集的IC50为0.45μM[2]。当与蛋白酶体抑制剂硼替佐米联合给药时,莫非唑酸略微增加硼替佐米对多发性骨髓瘤(MM)细胞系(NCI-H929和RPMI-8226)的细胞毒性作用,并影响MM细胞周期和凋亡[2]。

[体内研究]

莫非佐拉(1-30mg/kg；口服给药；一次)治疗可抑制小鼠腹腔注射苯基对苯醌引起的扭体[1]。动物模型：雌性ddY小鼠(4周龄,18-27g)注射苯基对苯醌(PQ)[1]剂量：1mg/kg,3mg/kg,10mg/kg,30mg/kg给药：口服；一次性结果：剂量依赖性地抑制注射PQ引起的小鼠扭体反应。

[参考文献]

[1]. K Goto, et al. Analgesic effect of mofezolac, a non-steroidal anti-inflammatory drug, against phenylquinone-induced acute pain in mice. Prostaglandins Other Lipid Mediat. 1998 Jul;56(4):245-54.

[2]. Maria Laura Pati, et al. Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Eur J Med Chem. 2019 Feb 15;164:59-76.

莫非佐酸物理化学性质

[ 密度 ]:
1.25g/cm3

[ 沸点 ]:
527.2ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₁₇NO₅

[ 分子量 ]:
339.34200

[ 闪点 ]:
272.7ºC

[ 精确质量 ]:
339.11100

[ PSA ]:
81.79000

[ LogP ]:
3.65290

[ 外观性状 ]:
浅黄色固体

[ 折射率 ]:
1.579

[ 储存条件 ]:
-20℃

莫非佐酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NY2101000

CHEMICAL NAME :: 5-Isoxazoleacetic acid, 3,4-bis(4-methoxyphenyl)-

CAS REGISTRY NUMBER :: 78967-07-4

LAST UPDATED :: 199612

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C19-H17-N-O5

MOLECULAR WEIGHT :: 339.37

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 :: 887 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 342 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 510 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - coma Behavioral - antipsychotic

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1528 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - coma Behavioral - antipsychotic

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 275 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - coma Behavioral - antipsychotic

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 545 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 800 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18200 mg/kg/91D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in spleen weight Nutritional and Gross Metabolic - changes in chlorine

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1820 mg/kg/91D-I

TOXIC EFFECTS :: Gastrointestinal - peritonitis Endocrine - changes in thymus weight Blood - changes in erythrocyte (RBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1650 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 - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2600 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Newborn - stillbirth

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2600 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) Reproductive - Effects on Embryo or Fetus - fetal death

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 600 mg/L

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 2),239,1990

莫非佐酸

莫非佐酸用途

莫非佐酸名称

莫非佐酸生物活性

莫非佐酸物理化学性质

莫非佐酸毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

莫非佐酸合成路线

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