酪里达唑

酪里达唑用途

西格列酮是一种有效的选择性PPARγ激动剂(EC50=3μM)。西格列酮抑制th17细胞的增殖和分化。西格列酮是一种口服降糖剂,在肥胖高血糖动物模型中具有活性。西格列酮在负鼠肾(OK)肾上皮细胞中诱导凋亡,同时激活p38 MAPK和凋亡诱导因子(AIF)的核转位[1][2][3][4]。

酪里达唑名称

[ CAS 号 ]:
74772-77-3

[ 中文名 ]:
环格列酮

[ 英文名 ]:
Ciglitazone

[中文别名 ]:

酪里达唑

[英文别名 ]:

Ciglitazone
UNII:U8QXS1WU8G
ciglitazonum
CIGLITIZONE
CIGLITLZONE
MFCD00865499
Flurofamide
AD-4533
ciglitazona
ADD 3878

酪里达唑生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 心血管疾病

信号通路 >> 细胞周期/DNA损伤 >> PPAR

[体外研究]

西格列酮(0-20μM；24小时)通过PPAR非依赖机制诱导细胞凋亡。西格列酮导致ROS的产生和细胞内Ca2+的增加[4]。

[体内研究]

在C57BL/6J ob/ob小鼠中,西格列酮(100 mg/kg/天；2天)引起血糖急剧下降。在使用100 mg/kg/天的西格列酮治疗41-44天的ob/ob小鼠中观察到胰岛β细胞的再颗粒化和胰腺胰岛素含量的增加[3]。

[参考文献]

[1]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996;39(3):665-668.

[2]. Kim DH, et al. Ciglitazone, a peroxisome proliferator-activated receptor gamma ligand, inhibits proliferation and differentiation of th17 cells. Biomol Ther (Seoul). 2015;23(1):71-76.

[3]. Chang AY, et al. Ciglitazone, a new hypoglycemic agent. I. Studies in ob/ob and db/db mice, diabetic Chinese hamsters, and normal and streptozotocin-diabetic rats. Diabetes. 1983;32(9):830-838.

[4]. Kwon CH, et al. Ciglitazone induces apoptosis via activation of p38 MAPK and AIF nuclear translocation mediated by reactive oxygen species and Ca(2+) in opossum kidney cells. Toxicology. 2009;257(1-2):1-9.

酪里达唑物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
504.5±23.0 °C at 760 mmHg

[ 熔点 ]:
130-131ºC

[ 分子式 ]:
C₁₈H₂₃NO₃S

[ 分子量 ]:
333.445

[ 闪点 ]:
258.9±22.6 °C

[ 精确质量 ]:
333.139862

[ PSA ]:
80.70000

[ LogP ]:
4.69

[ 外观性状 ]:
白色水晶般的固体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.568

[ 储存条件 ]:
2-8°C

酪里达唑MSDS

详细MSDS(安全技术说明书)

酪里达唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ5813700

CHEMICAL NAME :: 2,4-Thiazolidinedione, 5-((4-((1-methylcyclohexyl)methoxy)phenyl)methyl)-

CAS REGISTRY NUMBER :: 74772-77-3

LAST UPDATED :: 198910

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C18-H23-N-O3-S

MOLECULAR WEIGHT :: 333.48

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 950 mg/kg

SEX/DURATION :: female 1-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

REFERENCE :: SEIJBO Senten Ijo. Congenital Anomalies. (Nippon Senten Ijo Gakkai, c/o Kinki Daigaku Igakubu Kaibagaku Kyoshitsu, 380 Nishiyama, Sayama-cho, Mirami-Kawachi-gun, Osaka-fu, Japan) V.1-26, 1960-86. For publisher information, see CGANE7. Volume(issue)/page/year: 26,169,1986

酪里达唑安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;half-mask respirator (US);multi-purpose combination respirator cartridge (US)

[ 危害码 (欧洲) ]:
Xn

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

[ WGK德国 ]:
3

[ RTECS号 ]:
XJ5813700

酪里达唑文献

Developmental regulation and induction of cytochrome P450 2W1, an enzyme expressed in colon tumors.

PLoS ONE 10(4) , e0122820, (2015)

Cytochrome P450 2W1 (CYP2W1) is expressed predominantly in colorectal and also in hepatic tumors, whereas the levels are insignificant in the corresponding normal human adult tissues. CYP2W1 has been ...

Autonomous inhibition of apoptosis correlates with responsiveness of colon carcinoma cell lines to ciglitazone.

PLoS ONE 9(12) , e114158, (2014)

Colorectal cancer is a leading cause of mortality worldwide. Resistance to therapy is common and often results in patients succumbing to the disease. The mechanisms of resistance are poorly understood...

Thiazolidinedione insulin sensitizers alter lipid bilayer properties and voltage-dependent sodium channel function: implications for drug discovery.

J. Gen. Physiol. 138(2) , 249-70, (2011)

The thiazolidinediones (TZDs) are used in the treatment of diabetes mellitus type 2. Their canonical effects are mediated by activation of the peroxisome proliferator-activated receptor γ (PPARγ) tran...

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