FR 236924
(Synonyms: FR236924) 目录号 : GC12027
An activator of PKCε
Cas No.:28399-31-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
FR 236924 is a selective activator of PKC-ε [1].
PKC is a monomeric Ca2+- and phospholipid-dependent Ser/Thr protein kinase and plays an important role in growth factor-activated signaling and malignant transformation.
FR 236924 (DCP-LA) is a selective PKC-ε activator. In PC-12 cells, DCP-LA (10 nM-100 μM) activated PKC in a concentration dependent way with the maximal effect at 100 nM. In the cell-free system, DCP-LA (100 μM) significantly activated PKC-ε and exhibited >7-fold potency over other PKC isozymes (α,βI, βII, γ, δ, μ, η and ζ), suggesting that DCP-LA was a selective PKC-ε activator. DCP-LA exhibited the maximal effect on PKC-ε at 100 μM. The activation of PKC-ε induced by DCP-LA (100 μM) was inhibited by dioleoyl-phosphatidylserine in a concentration dependent way, suggesting that DCP-LA might bound to the phosphatidylserine binding site on PKC-ε. However, dioleoyl-phosphatidylserine increased DCP-LA (100 μM)-induced PKC-ε activation in a concentration dependent way, suggesting a different activation mechanism [1]. In Xenopus oocytes expressing α7 receptors, FR236924 (10 μM) induced a persistent increased α7 receptor responses to 144% via a PKC pathway. In rat hippocampal slices, FR236924 (10 nM to 10 μM) facilitated hippocampal neurotransmission [2].
In the hippocampus of rats, FR236924 induced glutamate release and facilitated hippocampal synaptic transmission through PKC [3].
References:
[1]. Kanno T, Yamamoto H, Yaguchi T, et al. The linoleic acid derivative DCP-LA selectively activates PKC-epsilon, possibly binding to the phosphatidylserine binding site. J Lipid Res, 2006, 47(6): 1146-1156.
[2]. Tanaka A, Nishizaki T. The newly synthesized linoleic acid derivative FR236924 induces a long-lasting facilitation of hippocampal neurotransmission by targeting nicotinic acetylcholine receptors. Bioorg Med Chem Lett, 2003, 13(6): 1037-1040.
[3]. Yamamoto S, Kanno T, Nagata T, et al. The linoleic acid derivative FR236924 facilitates hippocampal synaptic transmission by enhancing activity of presynaptic alpha7 acetylcholine receptors on the glutamatergic terminals. Neuroscience, 2005, 130(1): 207-213.
| Cas No. | 28399-31-7 | SDF | |
| 别名 | FR236924 | ||
| 化学名 | 8-((1R,2S)-2-(((1S,2R)-2-pentylcyclopropyl)methyl)cyclopropyl)octanoic acid | ||
| Canonical SMILES | OC(CCCCCCC[C@H]1[C@@H](C1)C[C@H]2[C@H](CCCCC)C2)=O | ||
| 分子式 | C20H36O2 | 分子量 | 308.5 |
| 溶解度 | DMF: 50 mg/ml,DMSO: 25 mg/ml,Ethanol: 10 mg/ml | 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 | 3.2415 mL | 16.2075 mL | 32.4149 mL |
| 5 mM | 0.6483 mL | 3.2415 mL | 6.483 mL |
| 10 mM | 0.3241 mL | 1.6207 mL | 3.2415 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。