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30748-29-9生产厂家

30748-29-9价格

30748-29-9

30748-29-9结构式
30748-29-9结构式
  • 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
  • 【用途一】
    抗炎药,用于风湿性和类风湿性关节炎等症的治疗

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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
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
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。
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

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

海关编码 2933990090
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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%
申报要素 品名, 成分含量, 用途, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期
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%