| CAS |
No.66575-29-9 |
| 中文名称 |
佛司可林(10mM in DMSO,无菌） |
| 英文名称 |
Forskolin(10mM in DMSO，Sterile） |
| 分子式 |
C22H34O7 |
| 分子量 |
410.5 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Adenylate Cyclase（AC）;FXR;PXR |
| 通路 |
GPCR & G Protein;Metabolic Enzyme&Protease |
| 背景说明 |
Forskolin是一种有效的腺苷酸环化酶激活剂。也是一种细胞内cAMP 形成的诱导剂。诱导多种细胞类型的分化并激活孕烷 X 受体 (PXR) 和 FXR。也可诱导细胞自噬。 |
| 生物活性 |
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart， and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.[1-8] |
| IC50 |
IC50: 41 nM (Adenylyl cyclase)[1]EC50: 0.5 μM (Adenylyl cyclase)[1] |
| In Vitro |
Forskolin (Coleonol) 也是前列腺癌 (PC) 细胞中有效的外泌体生物合成和/或分泌激活剂[8]。 Forskolin (Fsk) 是一种从锦紫苏中分离的天然二萜 forskholii，通过其催化亚基直接激活腺苷酸环化酶 (AC)，从而增加细胞内环磷酸腺苷 (cAMP) 的水平[1]。 Forskolin (Fsk) 影响人类 T 细胞系 (如 Kit 225 和 MT-2) 的增殖。Forskolin 处理以剂量依赖性方式抑制 Kit 225 和 MT-2 细胞的增殖，IC50 等于 ~5 μM Fsk。Forskolin 处理 (10-100 μM) 将 cAMPi 水平提高到基础水平的 5 到 20 倍，达到最大水平 50-100 μM Forskolin[6]。 |
| In Vivo |
Forskolin (Coleonol) 处理的 Mrp4-/- 小鼠显示 Ki67 阳性和裂解半胱天冬酶 3 阳性 EC 数量增加，周细胞覆盖量显著减少。在从 P7 到 P12 暴露于高氧 (75% 氧气) 的幼崽中，Mrp4-/- 小鼠显示无血管化视网膜区域显著增加[2]。 健康大鼠组平均血糖为 102.12±1.94 mg/dL，对照组为 101.25±3.56，Forskolin 组为 103±2.08。数据显示，Forskolin 组在研究结束时的血糖水平较低，根据所应用的统计检验具有显著差异 (p=0.03)[7]。 |
| 细胞实验 |
Quiescent Kit 225 or MT-2 cells are seeded into 96-well plates at 5×104 cells per well. Cells are then pretreated for 1 h with 1% DMSO (vehicle) or Forskolin at 1， 5， 10， 25， 50， and 100 μMconcentrations. The cells are stimulated with IL-2 and cultured for an additional 20 h at 37°C. Control cells are treated with 1% DMSO for 20 h. During the final 4 h of incubation， the cells are pulsed with [3H]thymidine at a concentration of 0.5 μCi/200 μL. Cells are harvested onto fiberglass filters and analyzed using liquid scintillation counting[2]. |
| 动物实验 |
Mice[3] C57BL/6J mice are used. Mrp4-knockout mice， which are established and repeatedly backcrossed to the C57BL/6J mice. Forskolin is injected intraperitoneally into neonatal mice at postnatal days 4 (P4) and 5 (P5). Mice injected with DMSO serve as the controls. The treated mice are euthanized at P6， and their retinas are isolated for whole-mount immunohistochemistry (IHC). The effect of different concentrations of Forskolin on the survival rate and retinal vasculature is first tested， and the optimal concentration is determined， 1.0 μg/50 μL (0.3 mg/kg) at P4 and 1.5 μg/50 μL (0.5 mg/kg) at P5， used to compare the retinal vascular phenotypes between WT mice and Mrp4-deficient mice. Rats[4] Male Wistar rats， aged 10-14 weeks old， with a mean weight of 300 g±50 g， are divided into four groups; 19 are experimentally induced to develop diabetes， and 8 are maintained in a healthy condition. Both diabetic and healthy rats receive no Forskolin (control)， or 6 mg/kg per day of Forskolin， administered orally for 8 weeks. Blood glucose levels are determined in each group before and after Forskolin treatment. The diabetic rats are tested two weeks after confirming the presence of diabetes (three weeks after the induction) and after eight weeks of the designated treatment. |
| 数据来源文献 |
[1]. Robbins JD， et al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52.
[2]. Matsumiya W， et al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35.
[3]. Mayati A， et al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115.
[4]. Awad JA， et al. Interactions of forskolin and adenylate cyclase. Effects on substrate kinetics and protection against inactivation by heat and N-ethylmaleimide. J Biol Chem. 1983 Mar 10;258(5):2960-5.
[5]. Seamon KB， et al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J Med Chem. 1983 Mar;26(3):436-9.
[6]. Ríos-Silva M， et al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52.
[7]. Rodriguez G， et al. Forskolin-inducible cAMP pathway negatively regulates T-cell proliferation by uncoupling the interleukin-2 receptor complex. J Biol Chem. 2013 Mar 8;288(10):7137-46.
[8]. Amrita Datta， et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
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