Troglitazone CAS: 97322-87-7
MF: C24H27NO5S
MW: 441.5
A potent antiproliferative, apoptosis inducer, antioxidant, and antiinflammatory agent.

Troglitazone (CAS 97322-87-7)

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应用; A potent antiproliferative, apoptosis inducer, antioxidant, and antiinflammatory agent
CAS号码: 97322-87-7
纯度: ≥98%
分子量: 441.5
分子式: C24H27NO5S
* 参考分析证明 大量特定数据 (包括水 含量).
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Troglitazone has been shown to be a potent antiproliferative and apoptosis inducer. This compound has displayed a capacity to inhibit growth of HCC cells via G1 phase cell cycle arrest through hypophosphorylation of Rb (retinoblastoma) protein and an increase of the cyclin-dependent kinase inhibitors, p21 and p27 proteins. In addition, Troglitazone has been reported to have profound antioxidant and antiinflammatory effects, and found to suppress L-type and receptor operated Ca2+ channel and PKC (protein kinase C). Experiments have shown Troglitazone to bind and activate PPARγ(peroxisome proliferator-activated receptor γ). PPARγ is mainly expressed in adipose tissue, one of the target tissues for insulin, but has subsequently been found to be expressed in vascular smooth muscle cells, endothelial cells, macrophages, and some cancer cells.


参考文献

1. Tsubouchi, Y., et al. 2000. Biochem. Biophys. Res. Commun. 270: 400-405. PMID: 10753637
2. Okura, T., et al. 2000. Eur. J. Pharmacol. 407: 227-235. PMID: 11068018
3. Fujiwara, T., et al. 2000. Life Sci. 67: 2405-2416. PMID: 11065164
4. Aljada, A., et al. 2001. J. Clin. Endocrinol. Metab. 86: 3250-3256. PMID: 11443197
5. Berger, J., et al. 2002. Annu. Rev. Med. 53: 409-435. PMID: 11818483
6. Yoshizawa, K., et al. 2002. Cancer. 95: 2243-2251. PMID: 12412180

物理状态 :
Solid
溶解度 :
Soluble in ethanol (>25 mg/ml) at 50° C, DMSO (>25 mg/ml), DMF (30 mg/ml), DMSO:PBS (1:6, pH 7.2) (0.1 mg/ml), and water (0.1 mg/ml) at 25° C.
保存 :
Store at -20° C
熔点 :
312.54° C (Predicted)
沸点 :
~657.0° C at 760 mmHg (Predicted)
密度 :
~1.3 g/cm3 (Predicted)
折射率 :
n20D 1.61 (Predicted)
IC50 :
Stimulatin PPARγg glucose transport: EC5050 = 1 µM (adipocytes); PPARγ: EC5050 = 780 nM (murine); PPARγ: EC5050 = 555 nM (human); Induces cell cycle arrest and apoptosis: EC5050 = 10 µM (cancer cell lines); Monoamine oxidase B: IC50 = 2.07 µM (human)
Ki 数据 :
Peroxisome proliferator-activated receptor gamma: Ki= 3.8 µM (human)
pK值 :
pKa: 6.35 (Predicted)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
2
RTECS :
XJ5813130
PubChem CID :
5591
默克索引 :
14: 9769
MDL 号码 :
MFCD00878416
SMILES :
CC1=C(C(=C2CCC(OC2=C1C)(C)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4)C)O

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PMID: # 31416829  2019. Biochem. J. 476: 2427-2447.

PMID: # 26313919  Myneni, VD. et al. 2015. Cell death & disease. 6: e1868.

PMID: # 24910239  Penner, N. et al. 2014. Drug Metab Lett. 8: 36-42.

PMID: # 22981620  Kim, JA. et al. 2012. Toxicology letters. 214: 175-81.

PMID: # 22365411  Kim, Y. et al. 2012. Eur J Med Chem. 50: 311-8.

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