Necrostatin 2 racemate (Synonyms: 7-Cl-O-Nec-1, Nec-1s) |
Catalog No.GC36711
One-Click Copy Product Info
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Necrostatin 2 racemate is a highly specific receptor-interacting protein kinase 1 (RIPK1) inhibitor that does not affect indoleamine 2,3-dioxygenase (IDO) activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 852391-15-2
Sample solution is provided at 25 µL, 10mM.
Necrostatin 2 racemate is a highly specific receptor-interacting protein kinase 1 (RIPK1) inhibitor that does not affect indoleamine 2,3-dioxygenase (IDO) activity[1]. Necrostatin 2 racemate is commonly used in research on inflammatory diseases (such as rheumatoid arthritis), neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), and organ protection[2, 3].
In vitro, treatment of pro-B exosomes+ lymphocytes with Necrostatin 2 racemate (1μM) for 48h significantly enhanced cytosporone B (10μM)-induced apoptosis, resulting in an average apoptosis rate of 63.14%, which was approximately 628% higher than that of the control group (10%)[4]. Pretreatment of wild-type bone marrow-derived macrophages (BMDMs) with Necrostatin 2 racemate (45μM), followed by co-treatment with heme and Pam3CSK4 (Pam3) for 48h, partially inhibited heme- and Pam3-induced cell death; this protective effect was further enhanced when combined with z-VAD-FMK (zVAD)[5]. Co-treatment of A549 and H358 cells with Necrostatin 2 racemate (10μM) and copper-based metal-organic frameworks (Cu-MOF) for 72h significantly reversed Cu-MOF-induced cytotoxicity and partially restored cell viability[6].
In vivo, daily intraperitoneal administration of Necrostatin 2 racemate (1.6mg/kg/day) in apolipoprotein E-deficient (ApoE-/-) mice, starting from angiotensin II (Ang II) infusion and continuing for 28 days, significantly alleviated abdominal aortic aneurysm (AAA) formation and reduced AAA incidence[7]. Daily intraperitoneal administration of Necrostatin 2 racemate (2mg/kg/day; once daily) in a neonatal mouse model of necrotizing enterocolitis (NEC), starting from NEC induction and continuing for 3 days, significantly improved survival rates, alleviated intestinal histopathological damage, and reduced the expression of pro-inflammatory cytokines (IL-1β, IL-17, TNF-α, and IFN-γ)[8].
References:
[1] YU J, ZHONG B, ZHAO L, et al. Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors Necrostatin-1 (Nec-1) and 7-Cl-O-Nec-1 (Nec-1s) are potent inhibitors of NAD(P)H: Quinone oxidoreductase 1 (NQO1)[J]. Free Radical Biology and Medicine, 2021, 173: 64-69.
[2] YU Z, JIANG N, SU W, et al. Necroptosis: a novel pathway in neuroinflammation[J]. Frontiers in Pharmacology, 2021, 12: 701564.
[3] MIFFLIN L, OFENGEIM D, YUAN J. Receptor-interacting protein kinase 1 (RIPK1) as a therapeutic target[J]. Nature Reviews Drug Discovery, 2020, 19(8): 553-571.
[4] GENTIMIR C A, GELEŢU G, CHELARU L, et al. Biochemical effects of TLRs, CXCL12, and necrosome activation on pro-B lymphocyte apoptosis in the presence of fibroblasts[J]. Romanian Journal of Oral Rehabilitation, 2022, 14(3).
[5] SUNDARAM B, PANDIAN N, MALL R, et al. NLRP12-PANoptosome activates PANoptosis and pathology in response to heme and PAMPs[J]. Cell, 2023, 186(13): 2783-2801.
[6] LI K, WU L, WANG H, et al. Apoptosis and cuproptosis co-activated copper-based metal-organic frameworks for cancer therapy[J]. Journal of Nanobiotechnology, 2024, 22(1): 546.
[7] WANG Q, ZHOU T, LIU Z, et al. Inhibition of Receptor-Interacting Protein Kinase 1 with Necrostatin-1s ameliorates disease progression in elastase-induced mouse abdominal aortic aneurysm model[J]. Scientific Reports, 2017, 7(1): 42159.
[8] LIU T, ZONG H, CHEN X, et al. Toll-like receptor 4-mediated necroptosis in the development of necrotizing enterocolitis[J]. Pediatric Research, 2022, 91(1): 73-82.
| Cell experiment [1]: | |
Cell lines | BMDMs (bone marrow-derived macrophages) |
Preparation Method | BMDMs were treated with a combination of 45μM Necrostatin 2 racemate (with or without zVAD), heme, and Pam3 for 48h, and the kinetics of cell death were monitored using the IncuCyte S3 or SX5 live-cell analysis system. |
Reaction Conditions | 45μM; 48h |
Applications | Necrostatin 2 racemate treatment partially reduced cell death in response to heme plus Pam3, compared with PBS control, and the addition of zVAD further reduced the cell death. |
| Animal experiment [2]: | |
Animal models | ApoE-/- mice (apolipoprotein E-deficient mice) |
Preparation Method | ApoE-/- mice received osmotic pumps that disbursed Ang II at 1000ng/kg/min. Daily injection of Necrostatin 2 racemate (1.6mg/kg/day; i.p.) started immediately following the pump implantation. Mice were euthanized 28 days after. The external aortic diameter was measured at the region showing maximum dilation with a digital caliper. Aneurysm incidence is defined as an increase of 50% or greater in the external width of the suprarenal aorta as compared with that of the infrarenal region. |
Dosage form | 1.6mg/kg/day; 28 days; i.p. |
Applications | Compared to the DMSO group, Necrostatin 2 racemate-treated mice showed significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (Nec-1s: 55.40 ± 13.08% vs. DMSO: 121.1 ± 16.44%, P < 0.05) as well as a reduced AAA incidence (from 90.5% to 33.3%). |
References: | |
| Cas No. | 852391-15-2 | SDF | |
| Synonyms | 7-Cl-O-Nec-1, Nec-1s | ||
| Canonical SMILES | ClC1=C2C(C(CC3C(N(C)C(N3)=O)=O)=CN2)=CC=C1 | ||
| Formula | C13H12ClN3O2 | M.Wt | 277.71 |
| Solubility | DMSO: ≥ 50 mg/mL (180.04 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6009 mL | 18.0044 mL | 36.0088 mL |
| 5 mM | 720.2 μL | 3.6009 mL | 7.2018 mL |
| 10 mM | 360.1 μL | 1.8004 mL | 3.6009 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)