Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Necrostatin 2 (also known as Necrostatin-2, Necrostatin-2 racemate, (±)-Necrostatin-2, 7-Cl-O-Nec-1 and Nec-1s) is a powerful necroptosis inhibitor with an EC50 of 50 nM. It is a racemic mixture that prevents the autophosphorylation of the receptor-interacting protein kinase 1 (RIPK1). A controlled caspase-independent cell death mechanism called necroptosis produces morphological characteristics that resemble necrosis. It can be brought on by TNF-alpha-treated human Jurkat T cells with a FADD-deficient variant. Additionally effective in an animal model of ischemic stroke, necrostatin 2 was. After being administered intravenously, necrostatin 2 showed moderate pharmacokinetic properties and quickly entered the central nervous system.
Targets |
Necroptosis; RIPK1
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ln Vitro |
Nec-1s is a potent inhibitor of RIPK1 and cellular necroptosis while lacking IDO inhibitory activity[1].
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ln Vivo |
Necrostatin 2 R-isomer(Nec-1s) is effective at minimizing brain injuries. It is a superior inhibitor that can be used in vivo and does not have a paradoxical sensitizing effect in TNF-induced lethality[1].
Necrostatin 2 R-isomer(Nec-1s) differs from Nec-1 in that it has a number of favorable pharmacokinetic and pharmacodynamic properties. Because of their lower in vivo and in vitro toxicity, Nec-1s have a safer safety profile than Nec-1[2]. |
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Enzyme Assay |
Necrostatin 2 (also known as Necrostatin-2, Necrostatin-2 racemate, (±)-Necrostatin-2, 7-Cl-O-Nec-1 and Nec-1s, is a potent necroptosis inhibitor with EC50 of 50 nM.
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Cell Assay |
Cells were treated with indicated concentrations of drug.
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Animal Protocol |
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References |
Molecular Formula |
C13H12CLN3O2
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Molecular Weight |
277.71
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Exact Mass |
277.0618
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Elemental Analysis |
C, 56.23; H, 4.36; Cl, 12.77; N, 15.13; O, 11.52
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CAS # |
852391-19-6
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Related CAS # |
Necrostatin 2 racemate;852391-15-2;Necrostatin 2 S enantiomer;852391-20-9
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Appearance |
Solid powder
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SMILES |
CN1C(=O)[C@H](NC1=O)CC2=CNC3=C2C=CC=C3Cl
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InChi Key |
WIKGAEMMNQTUGL-SNVBAGLBSA-N
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InChi Code |
InChI=1S/C13H12ClN3O2/c1-17-12(18)10(16-13(17)19)5-7-6-15-11-8(7)3-2-4-9(11)14/h2-4,6,10,15H,5H2,1H3,(H,16,19)/t10-/m1/s1
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Chemical Name |
(5R)-5-[(7-chloro-1H-indol-3-yl)methyl]-3-methylimidazolidine-2,4-dione
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Synonyms |
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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 |
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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 (9.00 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 (9.00 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 (9.00 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 | 3.6009 mL | 18.0044 mL | 36.0088 mL | |
5 mM | 0.7202 mL | 3.6009 mL | 7.2018 mL | |
10 mM | 0.3601 mL | 1.8004 mL | 3.6009 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.
Activity of Nec-1, Nec-1i and Nec-1s in an in vitro RIPK kinase assay and a cellular assay for necroptosis. Cell Death Dis . 2012 Nov 29;3(11):e437. td> |
Molecular docking of substrates, inhibitors and Nec-1 variants on human IDO. Cell Death Dis . 2012 Nov 29;3(11):e437. td> |
Molecular docking of substrates, inhibitors and Nec-1 variants on human IDO representing a similar docking pose for all ligands. Cell Death Dis . 2012 Nov 29;3(11):e437. td> |
Nec-1/1-M-Trp and Nec-1i, but not Nec-1s, inhibit IDO activity. Cell Death Dis . 2012 Nov 29;3(11):e437. td> |
Nec-1 and Nec-1i show a paradoxical dose response in TNF-induced SIRS. Cell Death Dis . 2012 Nov 29;3(11):e437. td> |
Nec-1s does not show a paradoxical dose response in TNF-induced SIRS. Cell Death Dis . 2012 Nov 29;3(11):e437. td> |