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- 文献和实验
- 技术资料
- CAS号：
1228690-19-4
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥242.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥600.0 |
| 规格： | 5mg | 产品价格： | ￥556.0 |
| 规格： | 10mg | 产品价格： | ￥848.0 |
| 规格： | 25mg | 产品价格： | ￥1080.0 |
| 规格： | 50mg | 产品价格： | ￥1352.0 |
| 规格： | 100mg | 产品价格： | ￥2152.0 |
| 规格： | 200mg | 产品价格： | ￥3024.0 |
Product Introduction
Bioactivity
| 名称 | AM966 |
| 描述 | AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release. |
| 细胞实验 | AM966 (Chem Scene, Monmouth Junction, NJ, USA) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.5%) before use.CHO-K1 cells are grown to 80% confluency in 12-well plates, serum-starved for 24 h and incubated in serum-free medium with AM966. After 21 h, [3H]thymidine (0.5 μCi/well) is added and the incubation is continued for 3 h. The medium is then removed, and the cells are placed on ice and washed twice with 1 mL of ice-cold PBS containing 5% trichloroacetic acid. Cells are solubilized and [3H]thymidine incorporation is determined by liquid scintillation counting. Assays are performed in triplicate. |
| 动物实验 | In fasted mice, received AM966 (10 mg/kg), which is prepared in water, by oral gavage. |
| 体外活性 | Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by either amitriptyline or mianserin. LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA1 over LPA2-5, with an IC50 value of 3.8±0.4 nM. AM966 inhibits LPA1-mediated chemotaxis of human A2058 melanoma cells (IC50=138±43 nM), IMR-90 human lung fibroblasts (IC50=182±86 nM) and CHO mLPA1 cells (IC50=469±54 nM). |
| 体内活性 | In a 3-day bleomycin model, AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 10 mg/mL (20.37 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 125 mg/mL (254.62 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (20.37 mM), Solution. 10% DMSO+90% Corn Oil : 2 mg/mL (4.07 mM), Sonication is recommended. |
| 关键字 | Lysophospholipid Receptor | LPLReceptor | LPL Receptor | LPL | LPAReceptor | LPA1 | LPA Receptor | Inhibitor | inhibit | AM-966 | AM966 | AM 966 |
| 相关产品 | Poloxamer 407 | Sphingosine-1-phosphate | S1PR1 modulator 1 | Siponimod | LX-2931 | Tyloxapol | SLP9101555 | Ki16198 | CAY10444 | CYM5181 | CYM50374 | ASP-4058 |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Highly Selective Inhibitor Library | NO PAINS Compound Library | GPCR Compound Library | Immunology/Inflammation Compound Library | Membrane Protein-targeted Compound Library | Orally Active Compound Library | Target-Focused Phenotypic Screening Library |
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文献和实验，而且它们的结构和反应活性与苯有相似之处，即有不同程度的芳香性，所以称为芳杂环化合物。 一、杂环化合物的分类和命名 杂环化合物可按杂环的骨架分为单杂环和稠杂环。单杂环又按环的大小分为五元杂环和六元杂环；稠杂环按其稠合环形式分为苯稠杂环和稠杂环。如表19-1所示。 杂环化合物的命名主要采用外文译音法，把杂环化合物的英文名称的汉字译音加“口”字旁表示。例如： 呋喃（furan） 吡啶（pyridine） 外文译音法是根据国际
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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