2. Immunology/Inflammation
  3. Complement System
  4. PMX 205

PMX 205 是一种有效的补体 C5a 受体 (C5aR; CD88) 拮抗剂。

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PMX 205 Chemical Structure

PMX 205 Chemical Structure

CAS No. : 514814-49-4

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.

IC50 & Target

C5aR[1]
体外研究
(In Vitro)

A complement activation product, C5a, is known to recruit and activate microglia and astrocytes in vitro by activation of a G protein-coupled cell-surface C5aR. In the MTT assay, in 24 h plate, it shows that all groups are significant when compared with negative control group. For PMX 205 (PMX205) group, the value recorded is in between 0.09893 to 0.2465, EP54 group, 0.02724 to 0.1748 and Tamoxifen group, the value recorded in between 0.09880 to 0.2464. For the 48 h plate of incubation time, only two groups show a significant result, which are PMX 205 and Tamoxifen. The values recorded are in between 0.04987 to 0.3273 and 0.5777 to 0.8551 respectively. For the 72 h plate, only one group shows a significant result, PMX 205 (antagonist group) with the value recorded in between 0.02136 to 0.5322[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PMX 205 (PMX205) is an orally active, selective C5aR antagonist. Animals treated with PMX 205 (1 mg/kg/day, oral) displays a significant extension of survival time and a reduction in end-stage motor scores, as compared with vehicle-treated rats. PMX 205-treated animals also display reduced levels of astroglial proliferation in the lumbar spinal cord. SOD1G93A rats are orally dosed with PMX 205 (1 mg/kg/day) from two time points (days 28 and 70) before the onset of major clinical symptoms. Both treatment groups have a significant extension in survival time compared with untreated rats (p=0.022, day 28; p=0.015, day 70), with no clear differences in outcomes between the two treatment regimens[2]. Tg2576 mice are treated with PMX 205 (PMX205) at 20 μg/mL in the drinking water (n=17) from 12 to 15 mo of age, the time frame at which there is a rapid accumulation of amyloid deposits in these animals. Untreated Tg2576 animals (n=11) are used as controls. After 3 mo, animals treated with PMX 205 show significantly less fibrillar plaque load (thioflavine reactivity) than do untreated animals. In 3×Tg mice, PMX 205 also significantly reduces hyperphosphorylated tau (69%)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

839.04

Formula

C45H62N10O6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Cell Assay
[1]

The mouse mammary tumor cell lines 4T1 are plated at a density 5.0×104 cells/ml/well of 96-multiwell plates in complete medium. After 24 h of incubation, the medium is changed with serum starve medium to synchronize the cell cycle and growth as to ensure that the cells reaches its plateau phase. After 24 h of serum-starving, cells are treated with 5 μL/well of 0.1 M of agonist, EP54, antagonist, PMX 205 and the positive control is treated with Tamoxifen drug. 5 μL/well of the 12 mM ck solution is added 5 h before reading is taken and about 50 μL/well of the SDS-HCL solution is added and mixed thoroughly using pipette 3 h before reading is taken. The MTT assay is assessed at different time point; 0, 24, 48 and 72 h at wavelength 570 nm respectively by using ELISA plate reader Infinite M200[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Rats[2]
Transgenic SOD1G93A rats expressing human mutant G93A SOD1 (NTac:SD-Tg SOD1G93A L26H) are used. Three experimental groups are chosen: untreated, PMX 205 treats from day 28 onward, and PMX 205 treats from day 70 onward. Animals are administered PMX 205 via drinking water (1 mg/kg/day) , from day 28 or day 70 onward; controls receive water only[2].
Mice[3]
Tg2576 mice are treated (starting at or after the initiation of plaque pathology) for 2-3 mo with PMX 205 given in the drinking water only (10-20 μg/mL, equivalent to ~3-6 mg/kg/day) or both in drinking water (10-20 μg/mL) and s.c. (1 mg/kg) twice weekly throughout the treatment period. Untreated transgenic animals of same age are used as controls. Nontransgenic littermates are similarly treated or not treated with the drug. 3×Tg mice are also treated with PMX 205 in the drinking water. Due to the low pathology of the males, only female mice of this strain are used for these studies[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

PMX 205 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • 冻干粉形式的重组蛋白如何溶解储存？

    1. 在打开盖子之前，先使用约 13000 rpm 的转速进行离心，20-30 s，将附着在管盖或管壁上的冻干粉收集到管底，以避免损失。 2. 以 10 μg 为例，先加 20 μL 我们赠送的复溶液，移液器吹打充分溶解。 3. 再加 80 μL 含载体蛋白（0.1% BSA, 5% HSA, 10% FBS, 或 5% 海藻糖中任一种）的缓冲液/培养基，移液器吹打混匀；最终浓度不低于 100 μg/mL。 4. 分装体积不少于 20 μL/管。 5. 分装后冻存于 -20ºC～-80ºC，可保存 3～6 个月。

  • 溶液形式的重组蛋白如何储存？

    1. 可以原产品储存，使用时再稀释。 2. 或者加含载体蛋白（0.1% BSA, 5, % HSA, 10% FBS, 或 5% 海藻糖中任一种）的缓冲液/培养基稀释，移液器吹打混匀，注意稀释后储存浓度不低于 100 μg/mL。 3. 分装体积不少于 20 μL/管。 4. 分装后冻存于 -20ºC～-80ºC，可保存 3～6 个月。

  • 为什么需要添加载体蛋白？

    载体蛋白通常被用于提高蛋白的稳定性，防止蛋白在冷冻或解冻过程中粘附在管壁上。离心管对蛋白有一定的吸附能力，这可能导致蛋白和管壁之间难以分离，导致溶液中蛋白的实际浓度下降，从而影响其活性。为减少这种损失，在长期保存重组蛋白产品之前，建议添加常用的载体蛋白溶液。

  • 载体蛋白种类和选择？

    0.1% BSA（牛血清白蛋白）、5% HSA（人血清白蛋白）、10% FBS（胎牛血清）或 5% 海藻糖，根据实验类型，若载体蛋白不影响研究结果，则可自选一种载体蛋白加到蛋白的储存液中。

  • 我收到的重组蛋白产品，什么也没看到，空空如也？

    冻干的体积大小受冻干前缓冲液组分、盐离子浓度、产品浓度等影响。由于工艺原因，蛋白冻干粉产品会呈现粉末状或肉眼不易观察到的透明薄膜状、胶冻状、雪花状，这些都是正常现象。此外，在运输过程中，冻干颗粒可能会分散，并粘附于瓶壁和瓶盖，肉眼无法清楚看到。收到产品后，请先离心，再按照冻干粉的重溶建议步骤，使用合适的缓冲液，重溶至说明书推荐的浓度，然后进行分装储存及使用。

  • 请问你们的重组蛋白都是有活性的吗？

    我们的重组蛋白可保证序列正确。至于蛋白是否有活性，取决于表达的序列是否包含活性区间。对于部分蛋白我们也会进行活性测试，并将数据公示于 COA 中。

  • 标签会对蛋白活性有影响吗？

    重组蛋白标签对蛋白的生物学活性影响存在未知结论，但对大部分检测应用中，重组蛋白的标签对蛋白本身生物学活性并无影响。MCE 对重组蛋白产品进行生物学活性检测，并将数据公示于 COA 中。

Keywords:

PMX 205514814-49-4PMX205PMX-205Complement SystemInhibitorinhibitorinhibit

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