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- CAS号:
301353-96-8
- 规格:
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mg | 产品价格: | ¥173.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥378.0 |
| 规格: | 5mg | 产品价格: | ¥364.0 |
| 规格: | 10mg | 产品价格: | ¥582.0 |
| 规格: | 25mg | 产品价格: | ¥1096.0 |
| 规格: | 50mg | 产品价格: | ¥1912.0 |
| 规格: | 100mg | 产品价格: | ¥3192.0 |
Product Introduction
Bioactivity
| 名称 | P7C3 |
| 描述 | P7C3 is a class of neuroprotective aminopropyl carbazoles which has been shown to block neuronal cell death in models of neurodegeneration. It was shown that P7C3 molecules additionally preserve axonal integrity after injury, before neuronal cell death occurs, in a rodent model of blast-mediated traumatic brain injury (TBI). This protective quality may be linked to the ability of P7C3 molecules to activate nicotinamide phosphoribosyltransferase, the rate-limiting enzyme in nicotinamide adenine dinucleotide salvage. |
| 激酶实验 | To assess the effect of compounds on auto-PARsylation of TNKS, 1 μM GST fusion protein containing the SAM domain and the PARP domain of TNKS2 (a.a. 872-1166) is mixed with 5 μM biotin-NAD+ and 2 μM XAV939 or LDW643 at 30°C for 2.5 hours. Samples are resolved by SDS-PAGE and probed with streptavidin AlexaFluor680. To assess PARsylation of axin, recombinant full-length TNKS2 (expressed/purified as a N-terminal His-tagged protein in bacteria) is incubated with GST-axin 1 (1-280) in the presence of biotin-NAD+ with or without XAV939. The products are resolved and probed with Streptavidin-HRP and imaged using a AlphaInnotech imager. To assess the effect of XAV939, IWR-1-enod, IWR-1-exo, and ABT-888 on auto-PARsylation of TNKS2, His-tagged full-length TNKS2 is incubated with 5 μM biotin-NAD+ and 3 mM of indicated compounds. The products are resolved and probed with Streptavidin-HRP. LC/MS-based high throughput auto-PARsylation assays for PARP1, PARP2, TNKS1, and TNKS2 are setup to monitor the formation of nicotinamide (a by-product of the PARsylation reaction) in the presence of small molecule inhibitors. |
| 体外活性 | In U2OS Cells, P7C3 protects cells from doxorubicin-mediated toxicity, and enhances the flux of nicotinamide through the NAMPT-mediated salvage pathway. [1] |
| 体内活性 | In mouse brain, P7C3 (40 mg/kg, p.o.) induces neurogenesis and enhances survival of newborn neurons. In npas3?/? mice, P7C3 (20 mg/kg/d, p.o.) increases the magnitude of neural precursor cell proliferation, and corrects morphological and electrophysiological deficits. [2] In the Ts65Dn mouse model of Down Syndrome, P7C3 restores hippocampal neurogenesis though a significant increase in total Ki67+, DCX+, and surviving BrdU+ cells. [3] |
| 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+40% PEG300+5% Tween 80+45% Saline : 8 mg/mL (16.87 mM), Suspension. Ethanol : 16 mg/mL (33.74 mM), Sonication is recommended. DMSO : 80 mg/mL (168.71 mM), Sonication is recommended. 10% DMSO+90% Saline : < 8 mg/mL (16.87 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | Parkinson's | P-7C3 | P7C3 | nicotinamide phosphoribosyltransferase | neuroprotective | neurodegenerative diseases | neurodegeneration | nerve | injury | Inhibitor | inhibit | disease | cell |
| 相关库 | Neuroprotective Compound Library | CNS-Penetrant Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Preclinical Compound Library | Anti-Neurodegenerative Disease Compound Library | Orally Active Compound Library | Anti-Metabolism Disease Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
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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