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Purity: ≥98%
Mdivi-1 (Mitochondrial Division Inhibitor 1; Mdivi 1; Mdivi1) is a potent selective and cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with the potential for treating stroke, myocardial infarction, and neurodegenerative disease. It inhibits DRP1 and Dnm1 with IC50s of 1-10 μM. Mdivi-1 inhibits apoptosis by inhibiting mitochondrial outer membrane permeabilization. Mdivi-1 treatment blocked apoptotic cell death in ischemic retina, and significantly increased RGC survival at 2 weeks after ischemia. Mdivi-1 is the first selective inhibitor of mitochondrial division dynamins and represents a class of therapeutics for stroke, myocardial infarction, and neurodegenerative diseases.
| ln Vitro |
Mdivi-1 has an estimated EC50 of 1–10 μM and inhibits Dnm1 GTPase activity in a dose-dependent manner. Mdivi-1 causes the enhanced Hill coefficient of GTP seen in Dnm1 GTP hydrolysis, as well as an increase in the apparent K0.5 of GTP and a decrease in the apparent Vmax of GTP hydrolysis [1]. Following apoptosis induction, cells treated with Mdivi-1 exhibited decreased cytochrome c release and decreased phosphatidylserine exposure, which is consistent with apoptosis inhibition and other studies that used other tactics to disrupt DRP1 activity [2]. In ischemic retina, Mdivi-1 induces apoptotic cell death [3].
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| ln Vivo |
mdivi-1 targets the mitochondrial fission DRP, Dnm1, in vivo. GMPPCP-dependent Dnm1 self-assembly is quantitatively blocked by Mdivi-1 at a concentration range that is comparable to its impact on mitochondrial fission in vivo [1]. In the normal mouse retina, Mdivi-1 (50 mg/kg, intraperitoneal injection) dramatically lowers the expression of GFAP protein [3].
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| References |
[1]. Cassidy-Stone A, et al. 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.
[2]. Tanaka A, et al. A chemical inhibitor of DRP1 uncouples mitochondrial fission and apoptosis. Mol Cell. 2008 Feb 29;29(4):409-10. [3]. Park SW, et al. 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 |
| Molecular Formula |
C15H10CL2N2O2S
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| Molecular Weight |
353.22
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| CAS # |
338967-87-6
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| SMILES |
O=C1N(C2=CC(OC)=C(Cl)C=C2Cl)C(NC3=C1C=CC=C3)=S
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| Chemical Name |
3-(2,4-dichloro-5-methoxyphenyl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one
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| Synonyms |
Mdivi-1; Mitochondrial Division Inhibitor 1; Mdivi 1; Mdivi1.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8311 mL | 14.1555 mL | 28.3110 mL | |
| 5 mM | 0.5662 mL | 2.8311 mL | 5.6622 mL | |
| 10 mM | 0.2831 mL | 1.4155 mL | 2.8311 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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