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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Boc-D-FMK is a cell-permeable, irreversible (covalent), and broad spectrum caspase inhibitor that blocks TNF-induced apoptosis with an IC50 of 39 µM.
Targets |
Caspase
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ln Vitro |
Apoptosis is a pathway of cell death orchestrated by a family of proteases called caspases. Reactive oxygen species (ROS) are produced when TNFα is activated, but Boc-D-fmk prevents this. With an IC50 of 39 µM[1], Boc-D-FMK blocks TNFα-induced apoptosis. Genistein-induced apoptosis of p815 cells is stopped by BocD-fmk at a concentration of 50 µM. The release of mitochondrial apoptotic factors is inhibited by BocD-fmk, according to confocal microscopy[2].
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ln Vivo |
In bile duct-ligated rats, Boc-D-FMK-fmk significantly reduces hepatocyte apoptosis and may increase survival after endotoxin challenge[3]. After receiving a single injection of Boc-D-FMK, MNs are long-term protected from root avulsion-induced death for more than 8 weeks, and the Boc-D-FMK-treated MNs are able to regenerate their axons into a PN graft that has been implanted and reinnervate the target muscle[4].
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References |
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Molecular Formula |
C11H18FNO5
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Molecular Weight |
263.26272726059
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Exact Mass |
263.12
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Elemental Analysis |
C, 50.19; H, 6.89; F, 7.22; N, 5.32; O, 30.39
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CAS # |
634911-80-1
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Related CAS # |
634911-80-1
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Appearance |
<31.2°C Solid,>31.2°C Liquid
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SMILES |
CC(C)(C)OC(=O)NC(CC(=O)OC)C(=O)CF
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InChi Key |
MXOOUCRHWJYCAL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C11H18FNO5/c1-11(2,3)18-10(16)13-7(8(14)6-12)5-9(15)17-4/h7H,5-6H2,1-4H3,(H,13,16)
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Chemical Name |
methyl 5-fluoro-3-[(2-methylpropan-2-yl)oxycarbonylamino]-4-oxopentanoate
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Synonyms |
BOC-D-FMK
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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) |
DMSO: ~100 mg/mL (~379.9 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.50 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 (9.50 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.7985 mL | 18.9926 mL | 37.9853 mL | |
5 mM | 0.7597 mL | 3.7985 mL | 7.5971 mL | |
10 mM | 0.3799 mL | 1.8993 mL | 3.7985 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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