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Mdivi 1

现货
Catalog No.
A4472
细胞渗透性DRP1/Dnm1选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 500.00
现货
50mg
¥ 2,000.00
现货

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Background

Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1). DRP1, a member of the dynamin family of large GTPases, mediates mitochondrial fission.

In vitro: The most efficacious inhibitor, mdivi-1 attenuates mitochondrial division in yeast and mammalian cells by selectively inhibiting the mitochondrial Drp1-mediated division dynamin. Mdivi-1 potently blocks Bid-activated Bax/Bak-dependent cytochrome c release from mitochondria [1].

In vivo: Mdivi-1 treatment blocked apoptotic cell death in ischemic retina, and significantly increased RGC survival at 2 weeks after ischemia. Moreover, Mdivi-1 treatment did not change this increase of Drp1 protein expression but significantly decreased GFAP protein expression [2].

Clinical trial: Currently no clinical data are available.

References:
[1] Cassidy-Stone A, Chipuk JE, Ingerman E, Song C, Yoo C, Kuwana T, Kurth MJ, Shaw JT, Hinshaw JE, Green DR, Nunnari J.  Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization. Dev Cell. 2008;14(2):193-204.
[2] Park SW, Kim KY, Lindsey JD, Dai Y, Heo H, Nguyen DH, Ellisman MH, Weinreb RN, Ju WK.  A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina. Invest Ophthalmol Vis Sci. 2011;52(5):2837-43.

文献引用

1. Chien L, Liang MZ, et al. "Mitochondrial therapy promotes regeneration of injured hippocampal neurons." Biochim Biophys Acta. 2018 Jun 15. pii: S0925-4439(18)30216-3. PMID:29913215

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt353.22
Cas No.338967-87-6
FormulaC15H10Cl2N2O2S
Solubility≥17.65mg/mL in DMSO, <2.434 mg/mL in EtOH, <2.12 mg/mL in H2O
Chemical Name3-(2,4-dichloro-5-methoxyphenyl)-2-sulfanylidene-1H-quinazolin-4-one
SDFDownload SDF
Canonical SMILESCOC1=C(C=C(C(=C1)N2C(=O)C3=CC=CC=C3NC2=S)Cl)Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

具有温度敏感性fzo1-1等位基因的酵母细胞

溶解方法

该化合物在DMSO中的溶解度大于17.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

50 μM

应用

Mdivi-1(50 μM)通过衰减Drp1的自组装抑制哺乳动物COS细胞中的线粒体分裂。Mdivi-1(50 μM)减弱凋亡过程中哺乳动物的线粒体分裂和Drp1自组装。FACS分析显示,Mdivi-1显著抑制STS诱导的非坏死细胞的膜联蛋白V染色,表明mdivi-1抑制细胞凋亡。

动物实验 [2]:

动物模型

C57BL/6小鼠

给药剂量

腹腔注射,50 mg/kg,60分钟

应用

Mdivi-1显著提高RGC存活率,中心区约为54%,中部为58%,外周区为48%。Mdivi-1治疗12小时,明显降低缺血性视网膜中的GFAP蛋白表达。Mdivi-1不改变平均动脉血压、体重、动物的外观或行为。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Cassidy-Stone A, Chipuk J E, Ingerman E, et al. Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization[J]. Developmental cell, 2008, 14(2): 193-204.

[2]. Park S W, Kim K Y, Lindsey J D, et al. A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina[J]. Investigative ophthalmology & visual science, 2011, 52(5): 2837-2843.

生物活性

Description Mdivi 1是一种细胞渗透性的线粒体分裂发动蛋白相关GTP酶(DRP1)和线粒体分裂发动蛋白I(Dnm1)选择性抑制剂。
靶点 DRP1 Dnm1        
IC50   1 - 10 ?M        

质量控制

化学结构

Mdivi 1

相关生物数据

Mdivi 1