Necrostatin 2 racemate (Nec-1s)

製品コードS8641 バッチS864103

印刷

化学情報

Chemical Structure Synonyms 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H12ClN3O2
分子量 277.71 CAS No. 852391-15-2
Solubility (25°C)* 体外 DMSO 56 mg/mL (201.64 mM)
Ethanol 56 mg/mL (201.64 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 56 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
in vitro

Nec-1s is a potent inhibitor of RIPK1 and cellular necroptosis while lacking IDO inhibitory activity[1].
in vivo

Nec-1s is effective in reducing brain injuries. It is a superior inhibitor suitable for use in vivo lacking a paradoxical sensitizing effect in TNF-induced lethality[1].

Nec-1s possesses several advantageous pharmacokinetic and pharmacodynamic characteristics in comparison to Nec-1. Safety profile of Nec-1s is also superior to that of Nec-1 for reduced in vivo and in vitro toxicity[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BMDMs
濃度 50 µM
反応時間 6 h
実験の流れ

Cells were treated with indicated concentrations of drug.
動物実験 動物モデル TNF-induced SIRS model (Female C57BL/6J WT mice)
投薬量 0.6 mg/kg and 6 mg/kg
投与方法 i.v.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] PubMed: 38297130
Inhibition of RIPK1 alleviating vascular smooth muscle cells osteogenic transdifferentiation via Runx2 [ iScience, 2024, 27(2):108766] PubMed: 38318355
NLRP6 induces RIP1 kinase-dependent necroptosis via TAK1-mediated p38MAPK/MK2 phosphorylation in S. typhimurium infection [ iScience, 2024, 27(4):109339] PubMed: 38500819
NLRP12-PANoptosome activates PANoptosis and pathology in response to heme and PAMPs [ Cell, 2023, 186(13):2783-2801.e20] PubMed: 37267949
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
p53 restoration in small cell lung cancer identifies a latent cyclophilin-dependent necrosis mechanism [ Nat Commun, 2023, 14(1):4403] PubMed: 37479684
EP1 activation inhibits doxorubicin-cardiomyocyte ferroptosis via Nrf2 [ Redox Biol, 2023, 65:102825] PubMed: 37531930
Epithelial Gab1 calibrates RIPK3-dependent necroptosis to prevent intestinal inflammation [ JCI Insight, 2023, 8(6)e162701] PubMed: 36795486
NHWD-1062 ameliorates inflammation and proliferation by the RIPK1/NF-κB/TLR1 axis in Psoriatic Keratinocytes [ Biomedicine & Pharmacotherapy, 2023, 114638] PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。