(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine
(Synonyms: CSTMP) 目录号 : GC41700
A stilbene derivative with antioxidant and anticancer activities
Cas No.:1000672-89-8
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
(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde (MDA) and decreases in superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities as well as increases constitutive nitric oxide synthase (cNOS) activity and nitric oxide (NO) production in HUVECs. CSTMP also induces cell death of A549 non-small cell lung cancer (NSCLC) cells in an IRE1α-dependent manner through induction of IRE1α-TRAF2-ASK1 complex-mediated endoplasmic reticulum (ER) stress and mitochondrial apoptosis.
| Cas No. | 1000672-89-8 | SDF | |
| 别名 | CSTMP | ||
| Canonical SMILES | CC1=C(C)N=C(C)C(/C=C/C2=CC=CC=C2Cl)=N1 | ||
| 分子式 | C15H15ClN2 | 分子量 | 258.8 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 2 mg/ml,Ethanol: 2 mg/ml | 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 | 3.864 mL | 19.3199 mL | 38.6399 mL |
| 5 mM | 0.7728 mL | 3.864 mL | 7.728 mL |
| 10 mM | 0.3864 mL | 1.932 mL | 3.864 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。
Cytoprotective effects of CSTMP, a novel stilbene derivative, against H2O2-induced oxidative stress in human endothelial cells
Pharmacol Rep 2011;63(6):1469-80.PMID:22358095DOI:10.1016/s1734-1140(11)70711-3.
A novel stilbene derivative, (E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP), was designed and synthesized based on the pharmacophores of tetramethylpyrazine (TMP) and resveratrol (RES). In the present study, we investigated the protective effects of CSTMP on vascular endothelial cells under oxidative stress and elucidated its molecular mechanisms. The radical scavenging activity of CSTMP was assessed by the DPPH test. Human Umbilical Vein Endothelial Cells (HUVECs) were exposed to 150 μM hydrogen peroxide (H(2)O(2)) for 12 h, resulting in a decrease of cell viability assessed by the MTT assay and an increase of apoptotic cells assessed by the nuclear staining assay and flow cytometry. The activities of lactate dehydrogenase (LDH), superoxide dismutase (SOD) and nitric oxide synthase (NOS) and the contents of malondialdehyde (MDA), reduced glutathione (GSH) and nitric oxide (NO) in cells were determined by commercial kits. The expression levels of pro-apoptotic factor caspase-3 and anti-apoptotic signal ERK1/2 were detected by western blot. The results showed that CSTMP had a moderate anti-oxidative effect against the DPPH test, which was less than RES. Co-incubation with CSTMP increased the cell viability, markedly reduced the LDH leakage from the cells and decreased the lipid peroxidation. These effects of CSTMP were accompanied by increasing activity of the endogenous antioxidant enzyme SOD, the level of GSH, the production of NO and cNOS activity. Moreover, CSTMP showed stronger effects on the inhibition of apoptosis, caspase-3 expression, and the activation of phosphorylated ERK1/2 compared to RES. Furthermore, CSTMP could inhibit the expression of phospho-JNK and phospho-p38 induced by H(2)O(2). These results suggest that CSTMP prevents H(2)O(2)-induced cell injury through anti-oxidation and anti-apoptosis via the MAPK and caspase-3 pathways.
CSTMP Exerts Anti-Inflammatory Effects on LPS-Induced Human Renal Proximal Tubular Epithelial Cells by Inhibiting TLR4-Mediated NF-κB Pathways
Inflammation 2016 Apr;39(2):849-59.PMID:26956469DOI:10.1007/s10753-016-0315-5.
(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP), a novel stilbene derivative, have been shown to have cytoprotective effects against H2O2-induced oxidative stress in human endothelial cells. However, little is known about its anti-inflammatory effects in lupus nephritis (LN). In the present study, we investigated the anti-inflammatory effects of CSTMP on lipopolysaccharide (LPS)-induced human renal proximal tubular epithelial cells (hRPTECs) and elucidated its molecular mechanisms. CSTMP significantly attenuated the cytotoxicity and suppressed the release of proinflammatory mediators, including iNOS, COX-2, TNF-α, IL-6, IL-8, CCL-2, ICAM-1, IL-1β, and MCP-1 in LPS-induced hRPTECs. In addition, CSTMP decreased the expression of TLR4 and its adapter molecules (MyD88, phosphorylation of TAK1, TRAF6, and IRAK1) and abolished its interactions with these adapter molecules in LPS-induced hRPTECs, resulting in an inhibition of the TLR4/MyD88/TAK1/ TRAF6/IRAK1 complex. Moreover, CSTMP also attenuated phosphorylation of IκB and IKK-α/β, and P50-NF-κB and P65-NF-κB translocation to nucleus in LPS-induced hRPTECs. These findings provided new insights to understand the mode of action of CSTMP in treatment of inflammatory diseases, such as LN.