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毛喉素 /Forskolin {[allProObj[0].p_purity_real_show]}

货号:A226193 同义名: 佛司可林 / Coleonol;Colforsin Ambeed 开学季,买赠积分,赢豪礼

Forskolin is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types with binding (IC50=41 nM) to and activation (EC50=0.5 μM) of type I adenylyl cyclase. It is commonly used to raise levels of cAMP in the research of cell physiology.

Forskolin 化学结构 CAS号:66575-29-9
Forskolin 化学结构
CAS号:66575-29-9
Forskolin 3D分子结构
CAS号:66575-29-9
Forskolin 化学结构 CAS号:66575-29-9
Forskolin 3D分子结构 CAS号:66575-29-9
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Forskolin 纯度/质量文件 产品仅供科研

货号:A226193 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AC EPAC1 EPAC2 PACAP receptor 其他靶点 纯度
Bithionol +

sAC, IC50: 4.0 μM

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SQ22536 {[allProObj[0].p_purity_real_show]}
ESI-09 ++

EPAC1, IC50: 3.2 μM

+++

EPAC2, IC50: 1.4 μM

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HJC0350 +++

EPAC2, IC50: 0.3 μM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Forskolin 生物活性

描述 Forskolin is a strong adenylate cyclase activator with an IC50 of 41 nM. Forskolin can activate adenylyl cyclase in broken cell preparations as well as in intact tissues, thereby resulting in marked increases of intracellular cyclic adenosine phosphate (cAMP) accumulation[1]. cAMP as a second messenger plays very important roles in biological processes. Forskolin elicits cellular responses which have been proposed to be dependent on cyclic AMP. In vitro studies have shown that forskolin significantly stimulated vasopressin (AVP) and oxytocin (OT) secretion from the rat neurohypophysis in a dose-dependent manner. Moreover, addition of forskolin to the rat hypotha-lamic SON in vitro increase cAMP accumulation, and Forskolin elicited a 3-fold greater increase in cyclic AMP in the neural lobe of the pituitary in vitro[2].
In human mesenchymal stromal cells (hMSCs), the use of Forskolin in different concentrations inhibits cell proliferation. At the same time, Forskolin induced alkaline phosphatase levels, bone-specific target genes, and secretion of insulin-like growth factor-1 in a manner related to concentration. The effect of forskolin on in vivo shows that bone formation ability significantly enhance after treatment of hMSCs with forskolin. In addition, 0.10mM forskolin displayed larger amounts of bone by pretreating hMSCs before implantation, compared with with 0.15 mM forskolin[3]. Importantly, Forskolin has been shown to have a number of relevant anticancer effects, such as the induction of mesenchymal-to-epithelial transition, the inhibition of proliferation, motility, and migration in many types of cancer cells, indicating its perspectives as an effective anticancer agent[4].
作用机制 Forskolin is a strong adenylate cyclase activator via an interaction with the catalytic subunit of adenylate cyclase, directly activating the adenylate cyclase enzyme and raising intracellular cAMP levels.

Forskolin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
3T3-L1 2.5/5 μM Function Assay 24 h  significantly decreases ATGL protein expression at all doses tested 25590597
3T3-L1 preadipocytes 10 μM  Function Assay 12 h induces CREB phosphorylation and C/EBPβ expression 25928058
AML-12 20 μM Function Assay 3 h upregulates the phosphorylation levels at Thr-411 and Ser-493 26048985
AML-12 20 μM Function Assay 1-8 h increases glucose production 26048985

Forskolin 动物研究

Dose Rat: 10 mg/kg - 30 mg/kg[5] (intragastric) Mice: 2.5 mg/kg - 10 mg/kg[6] (p.o.), 100 mg/kg[7] (p.o.)
Administration Intragastric, p.o.

Forskolin 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
NCT03390985 - Completed - -
NCT02586883 Idiopathic Dilation of the Bro... 展开 >>nchi 收起 << Not Applicable Recruiting April 2020 France ... 展开 >> Necker-Enfants Malades Hospital Recruiting Paris, France, 75015 Contact: Isabelle SERMET-GAUDELUS, MD, PhD    +33144494887    isabelle.sermet@nck.aphp.fr 收起 <<
NCT03455153 - Completed - United Kingdom ... 展开 >> Lindum Medical Practice Lincoln, Lincolnshire, United Kingdom, LN2 2JP Nettleham Medical Practice Lincoln, Lincolnshire, United Kingdom, LN2 2RS Birchwood Medical Practice Lincoln, Lincolnshire, United Kingdom, LN6 0QQ 收起 <<

Forskolin 参考文献

[1]Seamon KB, Padgett W, Daly JW. Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells. Proc Natl Acad Sci U S A. 1981;78(6):3363-7.

[2]Meeker RB, Michels KM, Hayward JN. Vasopressin and oxytocin regulation of cyclic AMP accumulation in rat hypothalamo-neurohypophysial explants in vitro. Neurosci Lett. 1990;114(2):225-30.

[3]Doorn J, Siddappa R, et al. Forskolin enhances in vivo bone formation by human mesenchymal stromal cells. Tissue Eng Part A. 2012;18(5-6):558-67.

[4]Sapio L, Gallo M, et al. The Natural cAMP Elevating Compound Forskolin in Cancer Therapy: Is It Time?. J Cell Physiol. 2017;232(5):922-927.

Forskolin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.18mL

2.44mL

1.22mL

24.36mL

4.87mL

2.44mL

Forskolin 技术信息

CAS号66575-29-9
分子式C22H34O7
分子量 410.5
别名 佛司可林 ;Coleonol;Colforsin;NSC 375489;NSC 357088;L 75-1362B;HL 362
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(255.78 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 12 mg/mL clear

PO 0.5% CMC-Na 100 mg/mL suspension

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