Phorbol

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Chemical Structure| 17673-25-5 同义名 : 4β-Phorbol; NSC 154778; (+)-Phorbol
CAS号 : 17673-25-5
货号 : A738144
分子式 : C20H28O6
纯度 : 99%+
分子量 : 364.43
MDL号 : MFCD00065450
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Phorbol is a highly toxic diterpene, and it's esters have important biological properties. Phorbol esters can stimulate calcium- and phospholipid-dependent protein kinase, leads to a marked attenuation of the ability of alpha 1-receptor agonists such as norepinephrine to stimulate the turnover of inositol phospholipids. The effect of phorbol esters on norepinephrine-stimulated inositol phospholipid turnover and alpha 1-receptor phosphorylation showed the same rapid time course with a t1/2 less than 2 min[3]. Phorbol esters inhibited the alpha 1-adrenoceptor-induced response; sub-nanomolar concentrations decreased the transient frequency, and higher concentrations abolished the transients. Phorbol esters were less effective in decreasing the frequency of [Arg8]-vasopressin-induced transients, and the inhibition could be overcome by high [Arg8]vasopressin concentrations[4]. In addition, phorbol esters stimulate insulin receptor phosphorylation, inhibit insulin-induced receptor phosphorylation and insulin action[5].
临床研究
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 ... 展开 >> Liverpool, United Kingdom, L9 7AL 收起 <<
NCT03448250 Breast Cancer Not Applicable Recruiting March 2020 Germany ... 展开 >> 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 收起 <<
NCT02137876 - Withdrawn(Subject recruitment ... 展开 >>was unsuccessful.) 收起 << - United States, Illinois ... 展开 >> Northwestern University Comprehensive Transplant Center Chicago, Illinois, United States, 60611 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL
参考文献

[1]Pagani A, Gaeta S, et al. An improved preparation of phorbol from croton oil. Beilstein J Org Chem. 2017 Jul 11;13:1361-1367.

[2]Matsuzawa Y, Kiuchi Y, et al. Activation of cytosolic phospholipase A2alpha by epidermal growth factor (EGF) and phorbol ester in HeLa cells: different effects of inhibitors for EGF receptor, protein kinase C, Src, and C-Raf. J Pharmacol Sci. 2009 Oct;111(2):182-92.

[3]Leeb-Lundberg LM, Cotecchia S, Lomasney JW, DeBernardis JF, Lefkowitz RJ, Caron MG. Phorbol esters promote alpha 1-adrenergic receptor phosphorylation and receptor uncoupling from inositol phospholipid metabolism. Proc Natl Acad Sci U S A. 1985 Sep;82(17):5651-5

[4]Woods NM, Cuthbertson KS, Cobbold PH. Phorbol-ester-induced alterations of free calcium ion transients in single rat hepatocytes. Biochem J. 1987 Sep 15;246(3):619-23

[5]Takayama S, White MF, Lauris V, Kahn CR. Phorbol esters modulate insulin receptor phosphorylation and insulin action in cultured hepatoma cells. Proc Natl Acad Sci U S A. 1984 Dec;81(24):7797-801