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洛索洛芬钠

洛索洛芬钠用途

Loxoprofen sodium 是一种具有镇痛、解热作用的非甾体类抗炎药。Loxoprofen sodium 是一种非选择性 COX 抑制剂,对 COX-1 和 COX-2 的 IC50 分别为 6.5 和 13.5 μM。

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洛索洛芬钠名称

[ CAS 号 ]:
80382-23-6

[ 中文名 ]:
洛索洛芬钠

[ 英文名 ]:
Loxoprofen sodium

[中文别名 ]:

洛索洛芬钠

[英文别名 ]:

Loxoprofen sodium
cs-600
loxoprofensodiumdihydrate
MFCD00941425
LOXOPROFEN NA
UNII:NDC2M7399S
Loxonin
sodium salt of Loxoprofen
Loxoprofen sodiuM hydrate
SodiuM Loxoprofen

洛索洛芬钠生物活性

[ 描述 ]:

Loxoprofen sodium 是一种具有镇痛、解热作用的非甾体类抗炎药。Loxoprofen sodium 是一种非选择性 COX 抑制剂,对 COX-1 和 COX-2 的 IC50 分别为 6.5 和 13.5 μM。

[ 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-1:6.5 μM (IC50)

COX-2:13.5 μM (IC50)

[体外研究]

洛索洛芬钠是一种抗炎前药(NSAID),是一种非选择性COX抑制剂,在人全血检测中COX-1和COX-2的IC50分别为6.5和13.5μM[1]。洛索洛芬(LOX)钠是一种非选择性环氧合酶抑制剂,广泛用于慢性和短暂性疾病引起的疼痛和炎症的研究。其醇代谢产物由羰基还原酶(CR)形成,由活性的反式LOX和不活跃的顺式LOX组成。此外,LOX钠也可以通过细胞色素P450(CYP)转化为非活性羟基化代谢物(OH-LOX)[2]。

[参考文献]

[1]. Riendeau D, et al. Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. Bioorg Med Chem Lett. 2004;14(5):1201-1203.

[2]. Paudel S, et al. Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. Pharmaceutics. 2019;11(9):479. Published 2019 Sep 16.

洛索洛芬钠物理化学性质

[ 沸点 ]:
417.9ºCat 760 mmHg

[ 分子式 ]:
C₁₅H₁₇NaO₃

[ 分子量 ]:
268.283

[ 闪点 ]:
220.7ºC

[ 精确质量 ]:
268.107544

[ PSA ]:
57.20000

[ LogP ]:
1.45170

[ 储存条件 ]:
室温，干燥

洛索洛芬钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CY1678845

CHEMICAL NAME :: Benzeneacetic acid, alpha-methyl-4-((2-oxocyclopentyl)methyl)-, sodium salt, dihydrate

CAS REGISTRY NUMBER :: 80382-23-6

LAST UPDATED :: 199412

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C15-H17-O3.Na.2H2-O

MOLECULAR WEIGHT :: 304.35

WISWESSER LINE NOTATION :: LVTJ B1R DY1&VO- &-NA- &QH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 857 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - bronchiolar constriction Lungs, Thorax, or Respiration - other changes

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 31,333,1993

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 145 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 245 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 285 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 155 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3030 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1020 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1070 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 740 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8 mg/kg

SEX/DURATION :: female 21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth)

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 36,1,1984

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洛索洛芬钠安全信息

[ 海关编码 ]:
2918300090

洛索洛芬钠合成路线

详细合成路线

洛索洛芬钠上下游产品

洛索洛芬钠上游产品

洛索洛芬钠下游产品

洛索洛芬钠海关

[ 海关编码 ]: 2918300090

[ 中文概述 ]:
2918300090 其他含醛基或酮基不含其他含氧基羧酸（包括酸酐、酰卤化物、过氧化物和过氧酸及该税号的衍生物）. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2918300090 other carboxylic acids with aldehyde or ketone function but without other oxygen function, their anhydrides, halides, peroxides, peroxyacids and their derivatives。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%