FR 236924 (Synonyms: FR 236924) |
カタログ番号GC12027 |
リノール酸誘導体である FR 236924 (FR236924) は、PKCε を選択的かつ直接的に活性化します。
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Cas No.: 28399-31-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- 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 | |
同義語 | FR 236924 | ||
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 | ||
Formula | C20H36O2 | M.Wt | 308.5 |
溶解度 | DMF: 50 mg/ml,DMSO: 25 mg/ml,Ethanol: 10 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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