非普拉宗_用途_密度_沸点_非普拉宗CAS号【30748-29-9】

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]。

[ 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。

[ 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

非普拉宗上游产品

非普拉宗下游产品

[ 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%

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Feprazone

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥1354.0/200mg ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：阿拉丁李高志

产品详情：非普拉宗

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