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苯扎隆

苯扎隆用途

苯扎龙(Fragivix)是一种有效的人尿酸转运蛋白1(hURAT1)抑制剂,在卵母细胞中的IC50为2.8μM。苯扎隆可降低血清尿酸水平[1]。

苯扎隆名称

[ CAS 号 ]:
1477-19-6

[ 中文名 ]:
苯扎隆

[ 英文名 ]:
Benzarone

[中文别名 ]:

[英文别名 ]:

(2-Ethylbenzofuran-3-yl)(4-hydroxyphenyl)methanone
Fragivix
Benzarone
Fagivil
Vasoc
Fragivil
Benzaron
Venagil

苯扎隆生物活性

[ 描述 ]:

苯扎龙(Fragivix)是一种有效的人尿酸转运蛋白1(hURAT1)抑制剂,在卵母细胞中的IC50为2.8μM。苯扎隆可降低血清尿酸水平[1]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> URAT1

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: 2.8 μM (hURAT1 in oocyte)[1]

[参考文献]

[1]. Wempe MF, et, al. Developing potent human uric acid transporter 1 (hURAT1) inhibitors. J Med Chem. 2011 Apr 28;54(8):2701-13.

苯扎隆物理化学性质

[ 密度 ]:
1.234g/cm3

[ 沸点 ]:
473.6ºC at 760mmHg

[ 熔点 ]:
124.3°

[ 分子式 ]:
C₁₇H₁₄O₃

[ 分子量 ]:
266.29100

[ 闪点 ]:
240.2ºC

[ 精确质量 ]:
266.09400

[ PSA ]:
50.44000

[ LogP ]:
3.93180

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
1.36E-09mmHg at 25°C

[ 折射率 ]:
1.638

[ 储存条件 ]:
通风低温干燥,与库房食品原料分开存放

[ 水溶解性 ]:
可溶于：甲醇

苯扎隆MSDS

苯扎隆毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OB2975000

CHEMICAL NAME :: Ketone, 2-ethyl-3-benzofuranyl p-hydroxyphenyl

CAS REGISTRY NUMBER :: 1477-19-6

BEILSTEIN REFERENCE NO. :: 0222901

LAST UPDATED :: 199701

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C17-H14-O3

MOLECULAR WEIGHT :: 266.31

WISWESSER LINE NOTATION :: T56 BOJ C2 DOR DQ

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 :: >12 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3400 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >12 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >12 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 154,94,1965

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >12 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52500 mg/kg/5W-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52500 mg/kg/30W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in calcium Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,949,1969 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1020 mg/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,961,1969

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,961,1969

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 600 mg/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 3,961,1969

苯扎隆安全信息

[ 海关编码 ]:
2932999099

苯扎隆合成路线

苯扎隆海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧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

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

苯扎隆文献

Interactions of urate transporter URAT1 in human kidney with uricosuric drugs.

Nephrology (Carlton.) 16(2) , 156-62, (2011)

Hyperuricaemia is a significant factor in a variety of diseases, including gout and cardiovascular diseases. The kidney plays a dominant role in maintaining plasma urate levels through the excretion p...

The EYA tyrosine phosphatase activity is pro-angiogenic and is inhibited by benzbromarone.

PLoS ONE 7(4) , e34806, (2012)

Eyes Absents (EYA) are multifunctional proteins best known for their role in organogenesis. There is accumulating evidence that overexpression of EYAs in breast and ovarian cancers, and in malignant p...

[Effect of benzarone on the oxygen consumption and the mechanical activity of vascular smooth muscle].

Arzneimittelforschung 33(2) , 211-4, (1983)

The influence of 2-ethyl-3-(4-hydroxy-benzoyl)-benzofurane (benzarone, Fragivic) on the energy metabolism of the wall of the rabbit common carotid artery and the rat portal vein was investigated by me...

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苯扎隆