米福贝特

米福贝特用途

Mifobate (SR-202) 是一种有效且特异性的 PPARγ 拮抗剂,可选择性的抑制噻唑烷二酮 (TZD) 诱导的 PPARγ 转录活性 (IC50=140 μM)。Mifobate 不影响 PPARα,PPARβ 或 FXR 的基础或配体刺激的转录活性。Mifobate 具有抗肥胖和抗糖尿病作用。

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米福贝特名称

[ CAS 号 ]:
76541-72-5

[ 中文名 ]:
米福贝特

[ 英文名 ]:
SR 202

[中文别名 ]:

[英文别名 ]:

Clenicor
SR-202
Mifobate

米福贝特生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> PPAR

研究领域 >> 代谢疾病

[ 靶点 ]

PPARγ:140 μM (IC50)

[体外研究]

米非特(100-400μM；24小时预处理)显著抑制6天后BRL 49653-和激素诱导的3T3-L1细胞脂肪细胞分化,呈剂量依赖性[1]。MIFOBATE能够与PPARγ特异性相互作用,并抑制其与共激活剂类固醇受体共激活因子-1(SRC-1)的激动剂依赖性相互作用。米非特(SR-202)抑制TZD刺激的促活化激素受体辅活化因子-1的募集。米非特阻断噻唑烷二酮类或地塞米松、胰岛素和3-异丁基-1-甲基黄嘌呤(IBMX)联合诱导的脂肪细胞分化[1]。

[体内研究]

米非特(400 mg/kg；喂养20天)提高ob/ob小鼠的胰岛素敏感性[1]动物模型：8周龄雄性ob/ob小鼠[1]剂量：400 mg/kg给药：饲料(食物混合液维持20天)结果：阻止葡萄糖浓度随时间的增加。

[参考文献]

[1]. Rieusset J, et al. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesityand antidiabetic activity. Mol Endocrinol. 2002 Nov;16(11):2628-44.

米福贝特物理化学性质

[ 密度 ]:
1.355g/cm3

[ 沸点 ]:
436.6ºC at 760 mmHg

[ 分子式 ]:
C₁₁H₁₇ClO₇P₂

[ 分子量 ]:
358.64900

[ 闪点 ]:
350.8ºC

[ 精确质量 ]:
358.01400

[ PSA ]:
99.91000

[ LogP ]:
4.24200

[ 外观性状 ]:
白色至灰白色的粉末或晶体

[ 折射率 ]:
1.494

[ 储存条件 ]:
-20°C，密封，干燥

米福贝特MSDS

详细MSDS(安全技术说明书)

米福贝特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TB8817000

CHEMICAL NAME :: Phosphoric acid, (4-chlorophenyl)(dimethoxyphosphinyl)methyl dimethyl ester

CAS REGISTRY NUMBER :: 76541-72-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C11-H17-Cl-O7-P2

MOLECULAR WEIGHT :: 358.67

WISWESSER LINE NOTATION :: 1OPO&O1&YR DG&OPO&O1&O1

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 :: 3200 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,271,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 580 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,271,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2 gm/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,271,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,271,1982

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米福贝特安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
TB8817000

[ 海关编码 ]:
2931900090

米福贝特合成路线

详细合成路线

米福贝特上下游产品

米福贝特上游产品

米福贝特下游产品

米福贝特海关

[ 海关编码 ]: 2931900090

[ 中文概述 ]:
2931900090. 其他有机-无机化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:AB(入境货物通关单,出境货物通关单). 最惠国关税:6.5%. 普通关税:30.0%

[ Summary ]:
2931900090. other organo-inorganic compounds. VAT:17.0%. Tax rebate rate:13.0%. Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward). MFN tariff:6.5%. General tariff:30.0%

米福贝特文献

Inhibitory effect of baicalin on iNOS and NO expression in intestinal mucosa of rats with acute endotoxemia.

PLoS ONE 8 , e80997, (2013)

The mechanism by which baicalin modulated the expression of inducible nitric oxide synthase (iNOS) and nitric oxide (NO) in the mucosa of distal ileum was investigated in a rat model of acute endo-tox...

Do peroxisome proliferation receptor-gamma antagonists have clinical potential as combined antiobesity and antidiabetic drugs?

Expert Opin. Investig. Drugs 12(4) , 713-6, (2003)

There is genetic evidence that reducing the activity of peroxisome proliferation receptor-gamma (PPAR-gamma) may increase insulin sensitivity. SR-202 is a selective antagonist at PPAR-gamma, which inh...

Antitumorigenic effect of Wnt 7a and Fzd 9 in non-small cell lung cancer cells is mediated through ERK-5-dependent activation of peroxisome proliferator-activated receptor gamma.

J. Biol. Chem. 281(37) , 26943-50, (2006)

The Wnt pathway is critical for normal development, and mutation of specific components is seen in carcinomas of diverse origins. The role of this pathway in lung tumorigenesis has not been clearly es...

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