Forskolin (Coleonol) 是一种有效的腺苷酸环化酶 (adenylate cyclase) 激活剂,对于 I 型腺苷酸环化酶,IC50为 41 nM,EC50为 0.5 μM。Forskolin 也是一种细胞内cAMP形成的诱导剂。Forskolin 诱导多种细胞类型的分化并激活孕烷 X 受体 (PXR) 和FXR。Forskolin 对心脏产生正性肌力作用,并具有血小板抗凝集和降压作用。Forskolin 也可诱导细胞自噬 (autophagy)。
生物活性 | Forskolin (Coleonol) is a potentadenylate cyclaseactivator with anIC50of 41 nM and anEC50of 0.5 μM fortype I adenylyl cyclase[1]. Forskolin is also an inducer of intracellularcAMPformation[2]. Forskolin induces differentiation of various cell types and activatespregnane X receptor (PXR)andFXR[3]. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also inducesautophagy[4][5]. |
IC50& Target | IC50: 41 nM (Adenylyl cyclase)[1] EC50: 0.5 μM (Adenylyl cyclase)[1] |
体外研究 (In Vitro) | Forskolin (Coleonol) is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells[8]. Forskolin (Fsk) is a naturally occurring diterpene isolated from Coleusforskholii, directly activates adenylyl cyclase (AC) through its catalytic subunit to increase intracellular levels of cyclic adenosine monophosphate (cAMP)[1]. Forskolin (Fsk) affects the proliferation of the human T-cell lines such as Kit 225 and MT-2. Forskolin treatment inhibits the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner with an IC50equal to ~5 μM Fsk. Forskolin treatment (10-100 μM) increases cAMPi levels ~5- to 20-fold above basal levels, which reache maximum levels between 50-100 μM Forskolin[6].
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体内研究 (In Vivo) | The Forskolin (Coleonol)-treated Mrp4-/-mice shows an increased number of Ki67-positive and cleaved caspase 3-positive ECs, a significant decrease in the amount of pericyte coverage, and a reduced number of empty sleeves. In pups exposed to hyperoxia (75% oxygen) from P7 to P12, the Mrp4-/-mice shows a significant increase in the unvascularized retinal area[2]. The average blood glucose in the healthy rat group is 102.12±1.94 mg/dL, 101.25±3.56 for control group and 103±2.08 in forskolin group. The data shows that glucose levels at the end of the study are lower in forskolin group, with a significant difference according to the statistical tests applied (p=0.03)[7].
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来源 | - Plants
- Compositae
- Gochnatia polymorpha(Less) Cabr.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(243.61 mM;Need ultrasonic) 配制储备液 1 mM | 2.4361 mL | 12.1803 mL | 24.3605 mL | 5 mM | 0.4872 mL | 2.4361 mL | 4.8721 mL | 10 mM | 0.2436 mL | 1.2180 mL | 2.4361 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 (protect from light)。-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: ≥ 2.5 mg/mL (6.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.09 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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%corn oil Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.09 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 25.0 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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