DCP-LA (FR236924) 是一种亚油酸衍生物，选择性地激活PKCε。DCP-LA 能够刺激 AMP 受体胞吐，并抑制蛋白磷酸酶-1 (PP-1) 和激活 Ca(2+)/钙调素依赖性蛋白激酶 II (CaMKII)。DCP-LA 能够抑制 caspase-3/-9 激活，以保护神经元免受到氧化应激诱导的细胞凋亡的影响。
| 生物活性 | DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activatesPKCε. DCP-LA activates Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulateAMPA receptorexocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-inducedapoptosis[1][2][3]. |
| IC50& Target[1][3] | |
体外研究
(In Vitro) | DCP-LA (100 nM; 15 min) activates cytosolic PKCε by binding to the phosphatidylserine binding/associating sites Arg50 and Ile89, without translocation towards the cell surface in PL-12 cells[1].
DCP-LA (10, 100, 100 nM; 10 min; 35 ℃) activates CaMKII and inhibits PP-1 in rat hippocampal neurons[2].
DCP-LA (100 nM; 20 min) increases expression of the receptors on the plasma membrane, responsible for potentiate AMPA receptor responses in rat hippocampal slices[2].
DCP-LA (100 nM; 10 min) results facilitation of hippocampal synaptic transmission[2].
DCP-LA (100 nM; 24 h) prevents theSodium nitroprusside(SNP, HY-10219) effect and rescues neurons from SNP-induced degradation[3].
DCP-LA (100 nM; 12 h) abolishes the caspase-3/9 activation induced bySodium nitroprusside(SNP, HY-10219) (1 mM)[3].
Cell Viability Assay[3] | Cell Line: | Rat cerebral cortical neurons | | Concentration: | 100 nM | | Incubation Time: | 24 hours; accompanied with 1 mMSodium nitroprusside(SNP) | | Result: | Prevented SNP-induced neuronal cell death. |
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体内研究
(In Vivo) | DCP-LA (1 mg/kg; p.o.; once daily; 7 d) exhibits a protective effect against ischemic brain damage, decreasing cerebral cortical defect due to middle cerebral artery (MCA) occlusion in mouse model[3].
| Animal Model: | Middle cerebral artery (MCA) occlusion in mouse model (male CB-17 mice, 5-8 weeks old)[3] | | Dosage: | 1 mg/kg | | Administration: | Oral gavage; once daily for 7 days; sacrificed mice on days 28 | | Result: | Significantly diminished degraded area due to cerebral infarction, with the rescued area reaching 82%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(16.21 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2415 mL | 16.2075 mL | 32.4149 mL | | 5 mM | 0.6483 mL | 3.2415 mL | 6.4830 mL | | 10 mM | 0.3241 mL | 1.6207 mL | 3.2415 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 0.5 mg/mL (1.62 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.62 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 0.5 mg/mL (1.62 mM); Suspended solution; Need ultrasonic
此方案可获得 0.5 mg/mL (1.62 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 0.5 mg/mL (1.62 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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