| CAS NO: | 28399-31-7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | Colourless oil |
| Storage | Store at -20°C |
| M.Wt | 308.5 |
| Cas No. | 28399-31-7 |
| Formula | C20H36O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
m.cnreagent.com