α-Amyloid Precursor Protein Modulator
目录号 : GC10343
α-Amyloid Precursor Protein Modulator 是一种细胞可渗透的苯并内酰胺衍生蛋白激酶 C (PKC) 激活剂，Ki 为 11.9 nM。
Cas No.:497259-23-1
Sample solution is provided at 25 µL, 10mM.
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α-Amyloid Precursor Protein Modulator is a benzolactam derived PKC activator.
Protein kinase C (PKC) belongs to a family of protein kinase enzymes involved in phosphorylating serine and threonine of other proteins. The PKC enzymes have been involved in regulating the function of other proteins. Protein kinase C plays an important role in several signal transduction cascades. Protein kinase C has been involved in modulating membrane structure events, mediating immune responses, regulating transcription, learning and memory, and regulating cell growth [2].
α-Amyloid Precursor Protein Modulator activated PKC with the Ki value of 11.9 nM for PKCα that efficiently enhanced non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblast AG06848. α-Amyloid Precursor Protein Modulator displayed a marked loss of tumor promoting activity [1].
References:
[1] Kozikowski A P, Nowak I, Petukhov P A, et al. New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPα[J]. Journal of medicinal chemistry, 2003, 46(3): 364-373.
[2] Stabel S, Parker P J. Protein kinase C[J]. Pharmacology & therapeutics, 1991, 51(1): 71-95.
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Cell experiment: |
24 h after plating 2×104 pheochromocytoma PC12 cells in each well of a 96 well plate, cells are incubated with TPPB at a series of concentration (0.1, 0.5, 1, 5, 10, 20 μM). Twelve to 24 h later, the original media is replaced with media containing MTT at a final concentration of 0.5 g/L for 4 h. Cell viability is evaluated with MTT assays[2]. |
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Animal experiment: |
Mice: Mice are 7 weeks old at the beginning of the treatments and are in the resting phase of the hair cycle. TPPB is applied once or else are applied twice weekly for a total of four applications. Two animals are treated at each dose of compound, and 72 h after the last application, the animals are euthanized. Two portions of treated skin are removed from each animal, fixed in neutral buffered formalin, and stained with hematoxylin and eosin for histological analysis[1]. |
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References: [1]. Kozikowski AP, et al. New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. J Med Chem. 2003 Jan 30;46(3):364-73. |
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| Cas No. | 497259-23-1 | SDF | |
| 化学名 | (2E,4E)-N-(5-(hydroxymethyl)-2-isopropyl-1-methyl-3-oxo-1,2,3,4,5,6-hexahydrobenzo[e][1,4]diazocin-8-yl)-5-(4-(trifluoromethyl)phenyl)penta-2,4-dienamide | ||
| Canonical SMILES | CC(C1C(NC(CO)CC2=C(C=CC(NC(/C=C/C=C/C3=CC=C(C(F)(F)F)C=C3)=O)=C2)N1C)=O)C | ||
| 分子式 | C27H30F3N3O3 | 分子量 | 501.54 |
| 溶解度 | 25.08mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9939 mL | 9.9693 mL | 19.9386 mL |
| 5 mM | 0.3988 mL | 1.9939 mL | 3.9877 mL |
| 10 mM | 0.1994 mL | 0.9969 mL | 1.9939 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet