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CAS No.: 16561-29-8

Phorbol 12-myristate 13-acetate/佛波酯 Catalog No. CSN11701

Synonyms: PMA;TPA;Phorbol myristate acetate

Phorbol 12-myristate 13-acetate is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.

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技术信息

生物活性

描述Protein kinase C (PKC) is a key molecule involved in cell growth, apoptosis, and differentiation. Phorbol 12-Myristate 13-Acetate (PMA) is an activator of certain types of PKC, including group A and group B isoforms^[3]. Stimulation with 1 μM PMA for 3 min resulted in promoted nucleotide exchange activity in 293T cells^[4]. In differentiated Caco-2 cells, pretreatment with 100 nM PMA for 5 min followed by 2h incubation with 10 nM 1,25(OH)₂D₃ resulted in a 2.6-fold increase in hCYP24A1 mRNA level compared to cells treated by 1,25(OH)₂D₃ alone. Incubation with 100 nM PMA for 30 min resulted in the activation of ERK1/2 and p38 kinase in Caco-2 cells, whereas pretreatment with the MEK inhibitor U0126 at 10, 20 or 100 μM completely inhibited ERK1/2 activation by PMA and partially suppressed PMA-induced p38 kinase activation. Cells pre-treated with 10 μM U0126 or 8 μM p38 kinase inhibitor SB202190 showed reduced enhancing effect of PMA on 1,25(OH)₂D₃-induced hCYP24A1 promoter activity^[5]. In both W/W^v genetically mast cell-deficient mice and congenic normal mice, repeated administration of PMA (5 μg, 3 times per week for 6 weeks) to the ear skin remarkably increased the number of dermal mast cells^[6].
作用机制PMA is a phorbol ester structurally analogous to diacylglycerol. It activates PKC isoforms by associating with their C1 domains^[7].
动物研究
剂量
Rat: 1.5 mg/kg - 3 mg/kg^[3] (intrarectal instillation); 230 μg/kg^[4] (i.v.)

给药途径
Intrarectal instillation, i.v.
临床研究

动物研究
剂量	Rat: 1.5 mg/kg - 3 mg/kg^[3] (intrarectal instillation); 230 μg/kg^[4] (i.v.)
给药途径	Intrarectal instillation, i.v.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01195272	Rheumatoid Arthritis	Phase 4	Completed	-	United Kingdom ... more >> Liverpool, United Kingdom, L9 7AL Collapse <<
NCT01195272	-	-	Completed	-	-
NCT02137876	-	-	Withdrawn(Subject recruitment ... more >>was unsuccessful.) Collapse <<	-	United States, Illinois ... more >> Northwestern University Comprehensive Transplant Center Chicago, Illinois, United States, 60611 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

16561-29-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C36H56O8

运输

蓝冰

分子量

616.83

别名

PMA;TPA;Phorbol myristate acetate;12-O-Tetradecanoylphorbol-13-acetate;NSC-262244;PD-616;RP-323;佛波酯

溶解度

DMSO	380.0 mg/mL (616.1 mM)
Water	insoluble
acetone	25.0 mg/mL (40.5 mM)

动物实验配方

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NCT01195272	Rheumatoid Arthritis	Phase 4	Completed	-	United Kingdom ... more >> Liverpool, United Kingdom, L9 7AL Collapse <<
NCT01195272	-	-	Completed	-	-
NCT02137876	-	-	Withdrawn(Subject recruitment ... more >>was unsuccessful.) Collapse <<	-	United States, Illinois ... more >> Northwestern University Comprehensive Transplant Center Chicago, Illinois, United States, 60611 Collapse <<
NCT00551746	Cardiovascular Disease	Not Applicable	Completed	-	United States, Utah ... more >> Intermountain Medical Center Murray, Utah, United States, 84157 Collapse <<
NCT03448250	Breast Cancer	Not Applicable	Recruiting	March 2020	Germany ... more >> Technical University of Dortmund, Leibniz Research Centre for Working Environment and Human Factors Recruiting Dortmund, Germany, 44139 Contact: Carsten Watzl, PhD +492311084233 watzl@ifado.de University Medical Center Leipzig, Department of Medical Psychology and Medical Sociology, Section Psychosocial Oncology Active, not recruiting Leipzig, Germany, 04103 Collapse <<
NCT00551746	-	-	Completed	-	-
NCT00364715	-	-	Completed	-	Taiwan ... more >> National Taiwan University Hospital Taipei, Taiwan, 100 Collapse <<

Phorbol 12-myristate 13-acetate/佛波酯 Catalog No. CSN11701

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