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| 25mg |
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Purity: ≥98%
Dynasore is a cell-permeable, reversible and non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2 (IC50 = 15 μM) with cardioprotective effects. It inhibits the mitochondrial dynamin Drp1 and has no effect against other small GTPase. Dynasore protects mitochondria and improves cardiac lusitropy in Langendorff perfused mouse heart.
| ln Vitro |
Dynasore inhibits dynamin1, dynamin2, and mitochondrial dynamin Drp1 GTPase activity, but not that of other small GTPases. When added, dynasore quickly prevents the creation of coated vesicles, thereby acting as a powerful inhibitor of the known dynamin-dependent endocytic pathway. This effect is seen within seconds. G-shaped, semi-formed pits and O-shaped, completely formed pits, which are trapped during pinch-off, are the two types of coated pit intermediates that accumulate during dynasore processing [1]. Human fetal neurons, astrocytes, primary reproductive tract cells, and epithelial and neural cells are all susceptible to HSV-1 and HSV-2 infection. Dynasore prevents these infections. When given eight hours after virus entrance, dynasore prevents newly generated viral proteins from leaving the nucleus and increases the amount of viral capsids that reach the nuclear pore [2]. Dynasore inhibits the rise in left ventricular end-diastolic pressure brought on either ischemia or reperfusion. Moreover, dynamicsore decreases infarct size and cardiac troponin I efflux upon reperfusion. Dynasore increased cardiomyocyte viability and survival in adult mouse cardiomyocytes grown under oxidative stress [3].
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| ln Vivo |
After spinal cord injury (SCI) in rats, dynasore dramatically reduced motor dysfunction at 3, 7, and 10 days. By preventing the activation of pathways leading to mitochondrial apoptosis and astrocyte proliferation in rat neurons following spinal cord damage, Dynasore greatly improves motor function [4].
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| References |
[1]. Macia E, et al. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50.
[2]. Mues MB, et al. Dynasore disrupts trafficking of herpes simplex virus proteins. J Virol. 2015 Jul;89(13):6673-84. [3]. Gao D, et al. Dynasore protects mitochondria and improves cardiac lusitropy in Langendorff perfused mouse heart. PLoS One. 2013 Apr 15;8(4):e60967. [4]. Li G, et al. Dynasore Improves Motor Function Recovery via Inhibition of Neuronal Apoptosis and Astrocytic Proliferation after Spinal Cord Injury in Rats. Mol Neurobiol. 2016 Nov 7. [5]. Liang Ma, et al. Discovery of the migrasome, an organelle mediating release of cytoplasmic contents during cell migration. Cell Res. 2015 Jan;25(1):24-38 |
| Molecular Formula |
C18H14N2O4
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| Molecular Weight |
322.31
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| CAS # |
304448-55-3
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| Related CAS # |
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| SMILES |
O=C(C1=C(O)C=C2C=CC=CC2=C1)N/N=C/C3=CC=C(O)C(O)=C3
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| InChi Key |
SYNDQCRDGGCQRZ-VXLYETTFSA-N
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| InChi Code |
InChI=1S/C18H14N2O4/c21-15-6-5-11(7-17(15)23)10-19-20-18(24)14-8-12-3-1-2-4-13(12)9-16(14)22/h1-10,21-23H,(H,20,24)/b19-10+
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| Chemical Name |
(E)-N-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide
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| Synonyms |
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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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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1026 mL | 15.5130 mL | 31.0260 mL | |
| 5 mM | 0.6205 mL | 3.1026 mL | 6.2052 mL | |
| 10 mM | 0.3103 mL | 1.5513 mL | 3.1026 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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