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PMX 205 Trifluoroacetate (514814-49-4 free base)

PMX 205 Trifluoroacetate (514814-49-4 free base)

产品编号 T12506   CAS T12506
别名: PMX 205 Trifluoroacetate

PMX 205 Trifluoroacetate is a potent complement antagonist of C5a receptor.

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PMX 205 Trifluoroacetate (514814-49-4 free base) Chemical Structure
PMX 205 Trifluoroacetate (514814-49-4 free base), CAS T12506
规格 价格/CNY 货期 数量
1 mg ¥ 700 待询
5 mg ¥ 1,750 待询

PMX 205 Trifluoroacetate (514814-49-4 free base) 的其他形式现货产品:

PMX 205 acetate(514814-49-4 free base)
其他形式的 PMX 205 Trifluoroacetate (514814-49-4 free base):
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产品目录号及名称: PMX 205 Trifluoroacetate (514814-49-4 free base) (T12506)
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参考文献
产品描述 PMX 205 Trifluoroacetate is a potent complement antagonist of C5a receptor.
体外活性 PMX205, which is an antagonist, gave more effects towards the cell as compared with the treatment of EP54.
体内活性 oral delivery of a cyclic hexapeptide C5a receptor antagonist (PMX205) for 2-3 mo resulted in substantial reduction of pathological markers such as fibrillar amyloid deposits (49-62%) and activated glia (42-68%) in two mouse models of AD. The reduction in pathology was correlated with improvements in a passive avoidance behavioral task in Tg2576 mice. In 3xTg mice, PMX205 also significantly reduced hyperphosphorylated tau (69%). These data provide the first evidence that inhibition of a proinflammatory receptor-mediated function of the complement cascade (i.e., C5aR) can interfere with neuroinflammation and neurodegeneration in AD rodent models, suggesting a novel therapeutic target for reducing pathology and improving cognitive function in human AD patients[3].
别名 PMX 205 Trifluoroacetate
分子量 953.06
分子式 C47H63F3N10O8
CAS No. T12506

存储

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

溶解度

DMSO: 100 mg/mL (104.93 mM)

H2O: 0.67 mg/mL (0.70 mM), Sonication is recommended.

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 1.0493 mL 5.2463 mL 10.4925 mL 26.2313 mL
5 mM 0.2099 mL 1.0493 mL 2.0985 mL 5.2463 mL
10 mM 0.1049 mL 0.5246 mL 1.0493 mL 2.6231 mL
20 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3116 mL
50 mM 0.021 mL 0.1049 mL 0.2099 mL 0.5246 mL
100 mM 0.0105 mL 0.0525 mL 0.1049 mL 0.2623 mL

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TargetMol Library Books参考文献

1. Kosni NN, et al. Expression of complement C5a receptor and the viability of 4T1 tumor cells following agonist-antagonist treatment. J Cancer Res Ther. 2016 Apr-Jun;12(2):590-6. 2. Woodruff TM, et al. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis. J Immunol. 2008 Dec 15;181(12):8727-34. 3. Fonseca MI, et al. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease. J Immunol. 2009 Jul 15;183(2):1375-83.

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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。

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Keywords

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