Necrostatin-7
(Synonyms: 5-[[3-(4-氟苯基)-1H-吡唑-4-基]亚甲基]-2-亚氨基-3-(2-噻唑基)-4-噻唑烷酮,Nec-7) 目录号 : GC44359
A necroptosis inhibitor
Cas No.:351062-08-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. Serine/threonine kinase activity of the death domain receptor-associated molecule RIP1 is thought to be essential for Fas ligand-induced and tumor necrosis factor-α (TNF-α) induced necrosis. Necrostatin-7 (Nec-7) is a necroptosis inhibitor that is structurally and biologically distinct from necrostatin-1, -3, -4, and -5 as it does not inhibit RIP1 kinase. Nec-7 may target an additional regulatory molecule in this pathway as it inhibits TNF-α-induced necroptosis in a FADD-deficient variant of human Jurkat T cells with an EC50 value of 10.6 μM.
| Cas No. | 351062-08-3 | SDF | |
| 别名 | 5-[[3-(4-氟苯基)-1H-吡唑-4-基]亚甲基]-2-亚氨基-3-(2-噻唑基)-4-噻唑烷酮,Nec-7 | ||
| Canonical SMILES | O=C(N(C1=NC=CS1)C(S/2)=N)C2=C\C3=CN([H])N=C3C4=CC=C(F)C=C4 | ||
| 分子式 | C16H10FN5OS2 | 分子量 | 371.4 |
| 溶解度 | DMSO: Soluble,Ethanol: Soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6925 mL | 13.4626 mL | 26.9251 mL |
| 5 mM | 0.5385 mL | 2.6925 mL | 5.385 mL |
| 10 mM | 0.2693 mL | 1.3463 mL | 2.6925 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Necrostatin-7 suppresses RANK-NFATc1 signaling and attenuates macrophage to osteoclast differentiation
Biochem Biophys Res Commun 2018 Sep 5;503(2):544-549.PMID:29800570DOI:10.1016/j.bbrc.2018.05.153.
Osteoclasts play a crucial role in osteolytic bone diseases, such as osteoporosis, rheumatoid arthritis, periodontitis, Paget's disease of bone and bone metastatic tumors. Therefore, controlling osteoclast differentiation and function has been considered a promising therapeutic strategy. Here, we show that necrostatin (Nec)-7, an inhibitor of programmed necrosis, strongly suppressed receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced osteoclastogenesis and bone resorption, without compromising macrophage colony-stimulating factor (M-CSF)-supported survival and growth of osteoclast precursor cells. Accordingly, Nec-7 significantly decreased the levels of RANKL-induced osteoclastogenic marker genes, such as cathepsin K. Mechanistically, Nec-7 neither affected MAPK nor NF-κB activation; however, it strongly inhibited the RANKL receptor (RANK) to nuclear factor of activated T cells c1 (NFATc1) signaling. Lentiviral expression of RANK in bone marrow-derived macrophages significantly restored osteoclastogenesis and NFATc1 amplification in Nec-7-treated cells. In this study, we revealed that Nec-7-sensitive pathways are crucially involved in osteoclast formation and function. Investigation of the molecular mechanism(s) through which Nec-7 inhibits RANK-NFATc1 signaling axis may lead to the development of new therapeutic strategies for bone disease.
[CARDIOPROTFETIVE EFECTS OF Necrostatin-7 IN THE RAT MODEL OF PERMANENT CORONARY OCCLUSION]
Ross Fiziol Zh Im I M Sechenova 2015 Apr;101(4):408-14.PMID:26336739doi
The cardioprotective effects of necroptosis inhibitor Necrostatin-7 were studied in the rat model of permanent coronary occlusion. It was found that intraperitoneal injection of Necrostatin-7 at a dose of 14.5 mg/kg 60 minutes prior to permanent left coronary artery occlusion reduced the amount of scar tissue and scar length in the left ventricle on the 21st day after surgery. In addition, pretreatment with Necrostatin-7 resulted in decreased plasma level of N-terminal pro-brain natriuretic peptide, which points to the improvement in left ventricular function.
Structure-activity relationship study of a novel necroptosis inhibitor, Necrostatin-7
Bioorg Med Chem Lett 2008 Sep 15;18(18):4932-5.PMID:18768316DOI:10.1016/j.bmcl.2008.08.058.
Necroptosis is a regulated caspase-independent cell death mechanism characterized by morphological features resembling non-regulated necrosis. Necrotatin-7 (Nec-7), a novel potent small-molecule inhibitor of necroptosis, is structurally distinct from previously described necrostatins (Nec-1, Nec-3, Nec-4 and Nec-5). Here, we describe a series of structural modifications and the structure-activity relationship (SAR) of the Nec-7 series for inhibiting necroptosis.