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Bezafibrate

CAS号

41859-67-0

分子式

C19H20ClNO4

主要靶点

PPAR

仅限科研使用

Cat No : CM00105

Print datasheet

Synonyms

inhibit|BM15075|BM-15075|BM 15075|Bezafibrate|Inhibitor|PPAR|PPARα|Peroxisome proliferator-activated receptors|苯扎贝特

验证数据展示

  • CAS No.: 41859-67-0

    Bezafibrate
    CAS#: 41859-67-0

产品信息

CAS号 41859-67-0
分子式 C19H20ClNO4
主要靶点 PPAR
主要通路 代谢|DNA 损伤和修复
分子量 361.82
纯度 99.82%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|BM15075|BM-15075|BM 15075|Bezafibrate|Inhibitor|PPAR|PPARα|Peroxisome proliferator-activated receptors|苯扎贝特

靶点活性

PPARδ (murine):110 μM|PPARα (murine):90 μM|PPARδ (human):20 μM|PPARγ (murine):55 μM|PPARα (human):50 μM|PPARγ (human):60 μM

体内活性

Bezafibrate与xPPARβ结合的EC50为5 μM。Bezafibrate转录激活Xenopus的PPARβ ,EC50=1 μM。

体外活性

Bezafibrate明显降低血浆甘油三酯和瘦素浓度,而无需修改白色脂肪组织PPARγ 水平或者 ob基因.服用Bezafibrate的野生型和PPARβ-null小鼠,性腺脂肪存储比对照组小很多(分别少2.8倍和 ~2.6倍),而同样方法喂养的PPARα-null的小鼠体内并没有这种效果.与对照组相比,Bezafibrate能够改变野生型,PPARβ-null 小鼠和 PPARα-null 小鼠体内mRNAs编码脂质代谢酶（例如AOX ,cytochrome P450 4A (CYP4A),LPL,ACS和 LCA D）.Bezafibrate能诱导大鼠附睾白脂肪组织中UCPs的表达,并且能通过直接诱导aco基因的表达（第7天14.5倍）和过氧化酶体脂肪酸β-氧化改变能量平衡.Bezafibrate治疗能够上调大鼠附睾白脂肪组织中M-CPT-I (4.5倍),脂肪酸移位酶(2.6倍) 和 Pref-1 (5.6倍)的mRNA水平. 与对照组相比,服用Bezafibrate会明显增加野生型和PPARβ-null小鼠的肝脏重量,而PPARα-null的小鼠肝脏重量不变.

溶解度

Ethanol:15 mg/mL (41.46 mM);DMSO:67 mg/mL (185.17 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

参考文献

1.Krey G, et al. Mol Endocrinol, 1997, 11(6), 779-791.
2.Cabrero A, et al. Diabetes, 2001, 50(8), 1883-1890.
3.Peters JM, et al. Biochim Biophys Acta, 2003, 1632(1-3), 80-89.
4.Vázquez M, et al. Mol Cell Biochem. 2001 Jan;216(1-2):71-8.
5.Franko A, et al. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266.
6.Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks[J]. Chemical Science. 2020, 11(7): 1775-1797.

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