80382-23-6

• 常用中文名：洛索洛芬钠
• 常用英文名：Loxoprofen sodium
• CAS号：80382-23-6
• 分子式：C₁₅H₁₇NaO₃
• 分子量：268.283
• 相关类别： 原料药 解热镇痛药 非甾抗炎药
• 发布时间：2018-07-01 17:54:09
• 更新时间：2024-01-02 15:38:21
• 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。

名称

• 中文名: 洛索洛芬钠
• 英文名: loxoprofen sodium hydrate
• 中文别名: 2-[4-(2-氧代环戊烷-1-基甲基)苯基]丙酸钠二水合物; 洛索洛芬钠
• 英文别名: Sodium 2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoate; Loxoprofen sodium; cs-600; loxoprofensodiumdihydrate; MFCD00941425; LOXOPROFEN NA; Benzeneacetic acid, α-methyl-4-[(2-oxocyclopentyl)methyl]-, sodium salt (1:1); UNII:NDC2M7399S; Loxonin; sodium salt of Loxoprofen; Loxoprofen sodiuM hydrate; SodiuM Loxoprofen; Unastin

物化性质

• 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

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.

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

安全

• 海关编码: 2918300090

合成路线

68767-14-6 ~98% 80382-23-6

文献：Yamakawa, Naoki; Suemasu, Shintaro; Matoyama, Masaaki; Kimoto, Ayumi; Takeda, Miho; Tanaka, Ken-Ichiro; Ishihara, Tomoaki; Katsu, Takashi; Okamoto, Yoshinari; Otsuka, Masami; Mizushima, Tohru Journal of Medicinal Chemistry, 2010 , vol. 53, # 21 p. 7879 - 7882

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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%