佛波醇12-十四酸酯13-乙酸酯
注：本產品僅用于科研，不可用于臨床
生物活性
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator[1][2]. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells
IC50 & Target
PKC 11.7 nM (EC50) | NF-κB
|
體外研究
(In Vitro)
In order to examine the role of PKC in p38MAPK phosphorylation, the cells are stimulated with the PKC activator, PMA (100 nM), which mimics the binding of DAG, the natural activator of PKC, to the C1 region of the PKCs. p38MAPK phosphorylation by PMA is observed in the two cell types similar to that observed by GnRH in αT3-1 cells, that is, a slow sustained activation (3.2-fold and 3.6-fold, respectively at 30 min). The paradoxical findings that PKCs activated by GnRH and PMA play a differential role in p38MAPK phosphorylation may be explained by differential localization of the PKCs. Basal, GnRH- and PMA- stimulation of p38MAPK phosphorylation in αT3-1 cells is mediated by Ca2+ influx via voltage-gated Ca2+ channels and Ca2+ mobilization, while in the differentiated LβT2 gonadotrope cells it is mediated only by Ca2+ mobilization[2].
THP-1 cells are differentiated into macrophage-like cells (THP-1 macrophages) by incubation in the presence of PMA (200 ng/mL; 1-5 days), which leads to a macrophage-like phenotype characterized by changes in morphology and increased cell surface expression of CD11 and CD14[3].
In the monocytic cell line THP-1, PMA results in a more differentiated phenotype than VD3, according to adherence, loss of proliferation, phagocytosis of latex beads, and expression of CD11b and CD14[5].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內研究
(In Vivo)
PMA is a PKC agonist, which reverses the damage induced by 5-hydroxydecanoic acid (5-HD). Thus, activation of the mitoKATP protected mitochondrial function in SOD and MDA via the PKC pathway[4].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
616.83
性狀
Solid
Formula
C36H56O8
中文名稱
佛波醇12-十四酸酯13-乙酸酯；(12-)十四酸佛波酯(-13-)乙酸鹽；佛波酯
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (162.12 mM; Need ultrasonic)
Ethanol : 100 mg/mL (162.12 mM; Need ultrasonic)
| 濃度溶劑體積質量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6212 mL | 8.1060 mL | 16.2119 mL |
| 5 mM | 0.3242 mL | 1.6212 mL | 3.2424 mL |
| 10 mM | 0.1621 mL | 0.8106 mL | 1.6212 mL |
請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。
請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊埾劝凑?In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.05 mM); Suspended solution; Need ultrasonic
- 3.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution
- 5.
請依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.05 mM); Suspended solution; Need ultrasonic
- 6.
請依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution
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