30748-29-9

• 常用中文名：非普拉宗
• 常用英文名：feprazone
• CAS号：30748-29-9
• 分子式：C₂₀H₂₀N₂O₂
• 分子量：320.385
• 相关类别： 原料药 解热镇痛药 非甾抗炎药
• 发布时间：2018-06-11 17:24:22
• 更新时间：2024-01-03 10:28:19
• 非普拉松(DA2370；Prenazone)是苯基丁酮(HY-B0230)的类似物,是一种非甾体抗炎剂,具有镇痛和解热作用。Feprazone通过抑制环氧合酶(COX)-2的活性而起作用。Feprazne通过减少线粒体活性氧(ROS)的产生来改善游离脂肪酸(FFA)诱导的氧化应激。Feprazone可降低MMP-2和MMP-9的表达。此外,Feprazene可抑制T3-L1细胞分化过程中的脂肪生成,增加脂肪分解。非普拉松还可用于研究动脉粥样硬化和肥胖[1][2][3]。

名称

• 中文名: 非普拉宗
• 英文名: Feprazone
• 中文别名: 1,2-二苯基-4-异戊烯基吡唑烷-3,5-二酮; 戊稀那宗
• 英文别名: feprazone; Prenazone; da2370; analud; 3,5-Pyrazolidinedione, 4-(3-methyl-2-buten-1-yl)-1,2-diphenyl-; methrazone; Grisona; MFCD00866063; 3,5-Pyrazolidinedione, 4-(3-methyl-2-butenyl)-1,2-diphenyl-; 4-Prenyl-1,2-diphenyl-3,5-pyrazolidindion; 4-(3-Methyl-2-buten-1-yl)-1,2-diphenyl-3,5-pyrazolidinedione; 4-(3-Methylbut-2-en-1-yl)-1,2-diphenylpyrazolidine-3,5-dione; Zepelin; EINECS 250-324-3; 4-(b-Isoamylenyl)-1,2-diphenyl-3,5-pyrazolidinedione; Nilatin; Naloven; Tabrien

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 437.2±28.0 °C at 760 mmHg
• 分子式: C₂₀H₂₀N₂O₂
• 分子量: 320.385
• 闪点: 178.7±16.4 °C
• 精确质量: 320.152466
• PSA: 40.62000
• LogP: 3.41
• 蒸汽压: 0.0±1.0 mmHg at 25°C
• 折射率: 1.600

生物活性

• 描述: 非普拉松(DA2370；Prenazone)是苯基丁酮(HY-B0230)的类似物,是一种非甾体抗炎剂,具有镇痛和解热作用。Feprazone通过抑制环氧合酶(COX)-2的活性而起作用。Feprazne通过减少线粒体活性氧(ROS)的产生来改善游离脂肪酸(FFA)诱导的氧化应激。Feprazone可降低MMP-2和MMP-9的表达。此外,Feprazene可抑制T3-L1细胞分化过程中的脂肪生成,增加脂肪分解。非普拉松还可用于研究动脉粥样硬化和肥胖[1][2][3]。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> 免疫及炎症 >> COX
  信号通路 >> 代谢酶/蛋白酶 >> MMP
• 靶点:

  COX, Reactive oxygen species, MMP[1]

• 体外研究: Feprazone(2.5-10μM；48 h)挽救FFAs刺激的人主动脉内皮细胞(HAEC)的细胞活力[1]。Feprazone(5,10μM；24 h)分别在5和10μM时将HAEC中的ROS生成降低至2.4倍和1.6倍,而300μM FFA将ROS生成增加3.4倍；还降低细胞因子CCL5、IL-6和IL-8以及MMP-2和MMP-9的mRNA表达和分泌[1]。Feprazone(5,10μM；6 h)降低TLR4和MyD88的活性,并降低p65的磷酸化和随后的NF-κB的活化[1]。Feprazone(30和60μM；7天)抑制分化的3个T3-L1细胞的脂肪生成；在3T3-L1脂肪生成过程中降低甘油三酯含量并增加脂肪分解[3]。细胞活力测定[1]细胞系：HAEC(用300μM FFA刺激)浓度：2.5、5和10μM孵育时间：48小时结果：在5和10µM时,细胞活力分别恢复到基线的81%和93%,而FFA将细胞活力降低到基线的63%。RT-PCR[1]细胞系：HAEC(用300μM FFA刺激)浓度：5和10μM孵育时间：24小时结果：以剂量依赖性方式降低细胞因子CCL5、IL-6和IL-8的mRNA表达和分泌。剂量依赖性地将VCAM-1和ICAM-1的表达分别降低到1.7倍和1.8倍,而FFA分别增加到2.8倍和3.4倍。Western Blot分析[1]细胞系：HAEC(用300μM FFA刺激)浓度：5和10μM孵育时间：6小时结果：降低TLR4和MyD88的表达,以及降低p65的磷酸化和随后的NF-κB的活化。
• 体内研究: 显著抑制HFD小鼠的脂肪细胞大小、内脏脂肪细胞组织重量和平均体重[3]。动物模型：雄性C57BL/6 N小鼠[高脂饮食(HFD)诱导的肥胖模型][3]剂量：75 mg/kg给药：(研究中未描述)结果：对照组、HFD组和HFD+Feprazone组小鼠的内脏脂肪细胞组织重量分别为0.38、3.51和2.37 g。对照组、HFD组和HFD+Feprazone组小鼠的平均体重分别为29.6、41.3和34.1 g。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UQ8530000 CHEMICAL NAME : 3,5-Pyrazolidinedione, 1,2-diphenyl-4-(3-methyl-2-butenyl)- CAS REGISTRY NUMBER : 30748-29-9 LAST UPDATED : 199612 DATA ITEMS CITED : 20 MOLECULAR FORMULA : C20-H20-N2-O2 MOLECULAR WEIGHT : 320.42 WISWESSER LINE NOTATION : T5VNNV EHJ BR& CR& E2UY1&1 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 : 1343 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,133,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 362 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,133,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 386 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 20,267,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1067 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,196,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 270 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,133,1979 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 374 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,133,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 180 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,196,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from stomach REFERENCE : YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 33,233,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 18 gm/kg/30D-C TOXIC EFFECTS : Gastrointestinal - ulceration or bleeding from stomach Liver - changes in liver weight Related to Chronic Data - death REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 64,255,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 98820 mg/kg/26W-C TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 64,255,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 6300 mg/kg/21D-I TOXIC EFFECTS : Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,226,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 16800 mg/kg/14W-I TOXIC EFFECTS : Cardiac - changes in heart weight Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,216,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 32400 mg/kg/30D-C TOXIC EFFECTS : Blood - normocytic anemia Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 64,255,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 54750 mg/kg/1Y-C TOXIC EFFECTS : Blood - normocytic anemia Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Liver - changes in liver weight REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 64,255,1982 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1320 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - delayed effects REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,149,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2640 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,149,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 180 mg/kg SEX/DURATION : female 17-22 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,164,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1620 mg/kg SEX/DURATION : female 17-22 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,164,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1560 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 - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,149,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 3120 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - abortion REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,149,1979

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海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
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Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%