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Neflamapimod

Neflamapimod

产品编号 T6089   CAS 209410-46-8
别名: VX-745

Neflamapimod (VX-745) 是一种可穿过血脑屏障的,高选择性的p38α抑制剂,对 p38α 的IC50值为 10 nM,p38β 的IC50值为 220 nM。它对 p38β 的特异性高 22 倍,具有抗炎活性。

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Neflamapimod Chemical Structure
Neflamapimod, CAS 209410-46-8
规格 价格/CNY 货期 数量
1 mg ¥ 196 现货
5 mg ¥ 455 现货
10 mg ¥ 667 现货
25 mg ¥ 1,430 现货
50 mg ¥ 2,580 现货
100 mg ¥ 3,220 现货
200 mg ¥ 4,690 现货
1 mL * 10 mM (in DMSO) ¥ 497 现货
产品目录号及名称: Neflamapimod (T6089)
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选择批次  
纯度: 99.75%
纯度: 99.02%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ.
靶点活性 p38α:10 nM, p38β:220 nM
体外活性 VX-745 selectively inhibits p38α and p38β MAPK with IC50 of 10 nM and 220 nM, respectively, but not p38γ MAPK and a large panel of other kinases, with IC50 larger than 20 μM. In a human peripheral blood mononuclear cell (PBMC) assay, VX-745 provides IC50 of 56 and 52 nM for IL-1β and TNFα, respectively. VX-745 blocks IL-6 and IL-8 production induced by IL-1 and TNFα, and COX-2 synthesis mediated by LPS and IL-1β. [1-3] VX-745 (60 nM-20 μM) inhibits IL-6 and VEGF secretion in bone marrow stromal cells (BMSCs), without affecting their viability. VX-745 also inhibits TNF-α-induced IL-6 secretion in BMSCs. VX-745 inhibits both multiple myeloma (MM) cell proliferation and IL-6 secretion in BMSCs triggered by adherence of MM cells to BMSCs, suggesting that VX-745 can inhibit paracrine multiple myeloma (MM) cell growth in the BM milieu and overcome cell adhesion-related drug resistance. [4]
体内活性 VX-745 is effective against adjuvant-induced arthritis (AA) in the rat with ED50 of 5 mg/kg. Histological scores for VX-745 in AA rats are 93% inhibition of bone resorption and 56% inhibition of inflammation. In the classical cartilage-induced arthritis model, VX-745 exhibits a dose-responsive decrease in severity score. [1-3] In a type II collagen-induced arthritis (CIA) mice model, VX-745 (2.5, 5, and 10 mg/kg) has 27%, 31%, and 44% improvement in the inflammatory scores, respectively, when compared to vehicle-treated mice. In addition, histological scores show a 32-39% protection of bone and cartilage erosion by VX-745. [5]
激酶实验 Spectrophotometric coupled-enzyme assay: The IC50 for the inhibition of p38α and p38β homologs are obtained by a spectrophotometric coupled-enzyme assay. A fixed concentration of enzyme (15 nM of p38α or p38β) is incubated with VX-745 in DMSO for 10 min. at 30 °C in 0.1 M HEPES buffer, pH 7.5, containing 10% glycerol, 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase, and 200 μM EGF receptor peptide (KRELVEPLTPSGEAPNQALLR). The reaction is initiated with 100 μM and 70 μM ATP for p38α and p38β assays, respectively. The decrease of absorbance at 340 nm is monitored to follow the rate of the reaction. IC50 is evaluated from the rate data as a function of the inhibitor concentration.
细胞实验 BMSCs (5 × 104 cells/well) or MM cells (3 × 104 cells/well) are incubated in 96-well culture plates in the presence or absence of VX-745 for 48 hours at 37 °C. DNA synthesis is measured by [3H]-thymidine ([3H]TdR) uptake. Cells are pulsed with [3H]TdR (0.5 μCi/well [.0185 MBq]) during the last 8 hours of 48-hour cultures. Growth inhibition of both MM cells and BMSCs by VX-745 is also assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance.(Only for Reference)
别名 VX-745
分子量 436.26
分子式 C19H9Cl2F2N3OS
CAS No. 209410-46-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 43.6 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2922 mL 11.4611 mL 22.9221 mL 57.3053 mL
5 mM 0.4584 mL 2.2922 mL 4.5844 mL 11.4611 mL
10 mM 0.2292 mL 1.1461 mL 2.2922 mL 5.7305 mL
20 mM 0.1146 mL 0.5731 mL 1.1461 mL 2.8653 mL
50 mM 0.0458 mL 0.2292 mL 0.4584 mL 1.1461 mL
100 mM 0.0229 mL 0.1146 mL 0.2292 mL 0.5731 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Decicco C, et al. American Chemical Society, 2000, IDDB3. 2. Haddad JJ, Curr Opin Investig Drugs, 2001, 2(8), 1070-1076. 3. Salituro FG, et al. 27th National Medicinal Chemistry Symposium, 2000, June 16. 4. Hideshima T, et al. Blood, 2003, 101(2), 703-705. 5. Duffy JP, et al. ACS Med Chem Lett, 2011, 2(10), 758-763. 6. Pradal J, et al. Intra-articular bioactivity of a p38 MAPK inhibitor and development of an extended-release system. Eur J Pharm Biopharm. 2015 Jun;93:110-7. 7. Alam JJ. Selective Brain-Targeted Antagonism of p38 MAPKα Reduces Hippocampal IL-1β Levels and Improves Morris Water Maze Performance in Aged Rats. J Alzheimers Dis. 2015;48(1):219-27.
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相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抗癌临床化合物库 高选择性抑制剂库 抗癌药物库 抗卵巢癌化合物库 自噬库 成骨分子库 激酶抑制剂库 抗衰老化合物库 MAPK 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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g
给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Neflamapimod 209410-46-8 Autophagy MAPK p38 MAPK Inhibitor VX 745 VX-745 VX745 inhibit inhibitor

 

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