| 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 | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Necroptosis; RIPK1
This compound targets receptor-interacting protein kinase 1 (RIPK1), a key regulator of necroptosis, a regulated caspase-independent cell death pathway morphologically resembling necrosis. By inhibiting RIPK1 autophosphorylation, Necrostatin 2 R-isomer blocks the necroptotic signaling pathway. It is effective at minimizing brain injuries. |
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| ln Vitro |
Nec-1s is a potent inhibitor of RIPK1 and cellular necroptosis while lacking IDO inhibitory activity[1].
In vitro, Necrostatin 2 R-isomer is a potent inhibitor of necroptosis with an EC50 of 50 nM. It inhibits RIPK1 autophosphorylation and blocks the downstream signaling cascade that leads to necroptotic cell death. Detailed in vitro activity data in specific cell lines are not provided. |
| 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]. In vivo, Necrostatin 2 R-isomer is effective at minimizing brain injuries. It is a superior inhibitor that can be used in vivo and does not have the paradoxical sensitizing effect in TNF-induced lethality that is observed with some other necroptosis inhibitors. It reduces inflammation by modulating apoptosis. |
| 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.
RIPK1 inhibitory activity is determined using cell-free kinase assays with recombinant RIPK1 enzyme, a peptide substrate, and ATP. Phosphorylation of the substrate is measured, and IC50 or EC50 values are calculated from dose-response curves. |
| Cell Assay |
Cells were treated with indicated concentrations of drug.
Cell-based assays for Necrostatin 2 R-isomer use cell lines that are sensitive to necroptotic stimuli (e.g., TNF-α + zVAD + SM-164). Cells are treated with the compound, and cell death is measured by propidium iodide staining or LDH release. Inhibition of RIPK1 autophosphorylation is assessed by Western blot. |
| Animal Protocol |
In vivo animal studies for Necrostatin 2 R-isomer are conducted in mouse models of brain injury or TNF-induced systemic inflammatory response syndrome (SIRS). The compound is administered, and tissue injury, inflammation markers, and survival are assessed. Its lack of paradoxical sensitizing effect makes it suitable for in vivo use. |
| ADME/Pharmacokinetics |
Necrostatin 2 R-isomer has the molecular formula C₁₃H₁₂ClN₃O₂ with a molecular weight of 277.71. It is the R-isomer of (±)-Necrostatin-2. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not disclosed in the available references.
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| Toxicity/Toxicokinetics |
No specific toxicity data are detailed in the available references. However, the compound is described as a superior inhibitor that can be used in vivo without the paradoxical sensitizing effect in TNF-induced lethality, suggesting a favorable safety profile compared to other necroptosis inhibitors.
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| References | |
| Additional Infomation |
Necrostatin 2 R-isomer (also known as Nec-1s, 7-Cl-O-Nec-1) is a research compound not yet approved for clinical use. It is a potent inhibitor of necroptosis that targets RIPK1. Its lack of paradoxical sensitizing effect makes it a valuable tool for studying necroptosis in vivo and for exploring therapeutic applications in diseases where necroptosis plays a role, such as brain injury and inflammatory disorders.
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| Molecular Formula |
C13H12CLN3O2
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| Molecular Weight |
277.71
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| Exact Mass |
277.062
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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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| PubChem CID |
11288934
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| Appearance |
White to light yellow solid powder
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| LogP |
1.491
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
403
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C([C@H]1NC(=O)N(C)C1=O)C1=CNC2C(=CC=CC1=2)Cl
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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.
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