Mdivi-1

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Chemical Structure| 338967-87-6 同义名 : Mitochondrial division inhibitor 1
CAS号 : 338967-87-6
货号 : A252480
分子式 : C15H10Cl2N2O2S
纯度 : 99%+
分子量 : 353.223
MDL号 : MFCD00974506
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 155 mg/mL(438.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • Dynamin

    Dnm1 GTPase, IC50:1 μM-10 μM
描述 Mdivi-1, derivative of quinazolinone, is a selective inhibitor of mitochondrial division by targeting Dnm1 (dynamin-1) and DRP (dynamin-related protein). In mammalian cells (COS cell), mdivi-1 inhibits mitochondrial division with IC50 of 50 μM by specially inhibiting DRP1 activity, and in Hela cell, mdivi-1 impedes apoptosis early in the intrinsic pathway by attenuating Bak/Bax dependent MOMP (mitochondrial outer membrane permeabilization)[3]. It has been shown to reduce seizure activity and increase survival of KA-reduced mice intravenously injected of 20 mg/kg mdivi-1 by protecting mitochondrial morphology and attenuating cell death in the hippocampus[4]. In the study of ischemia reperfusion injury, mdivi-1 can protect against ischemia reperfusion injury of spinal cord neurons and mitochondrial dysfunction in vivo through activating BK channels dependently in SD rat which were treated with intravenous bolus of 1 mg/kg[5]. The function of mdivi-1 is also reflected in the protection of ischemic retina. Research has shown that mdivi-1 can reverse cell apoptosis caused by transient retinal ischemia and significantly increase the number and survival of retinal ganglia cells by approximately 54% in 3-month-old C57BL/6 mice (intraperitoneal injection, 50 mg/kg). In addition, mdivi-1 treatment did not affect the increase of Drp1 protein expression, but obviously down-regulate the expression of GFAP[6]. Multiple roles of mdivi-1, such as reduces animal blood pressure, alleviate traumatic brain injury induced brain damage[7], and protect against doxorubicin-induced cardiotoxicity, have confirmed by relevant experiments[8]. In general, mdivi-1 provides a new treatment for stroke, myocardial infarction and neurodegenerative diseases.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.16mL

2.83mL

1.42mL

28.31mL

5.66mL

2.83mL
参考文献

[1]14(2):193-204.

[2]17(1):33.

[3]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 Feb;14(2):193-204.

[4]Kim H, Lee JY, Park KJ, Kim WH, Roh GS. A mitochondrial division inhibitor, Mdivi-1, inhibits mitochondrial fragmentation and attenuates kainic acid-induced hippocampal cell death. BMC Neurosci. 2016 Jun 10;17(1):33.

[5]Liu JM, Yi Z, Liu SZ, Chang JH, Dang XB, Li QY, Zhang YL. The mitochondrial division inhibitor mdivi-1 attenuates spinal cord ischemia-reperfusion injury both in vitro and in vivo: Involvement of BK channels. Brain Res. 2015 Sep 4;1619:155-65.

[6]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 Apr 27;52(5):2837-43.