产品说明书
Forskolin
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同义名 : | 佛司可林 ;Coleonol;Colforsin;NSC 375489;NSC 357088;L 75-1362B;HL 362 |
| CAS号 : | 66575-29-9 | |
| 货号 : | A226193 | |
| 分子式 : | C22H34O7 | |
| 纯度 : | 98% | |
| 分子量 : | 410.5 | |
| MDL号 : | MFCD00082317 | |
| 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 |
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| 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 |
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| 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 |
| 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]. |
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| 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. | ||
| 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 |
| 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 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.44mL 0.49mL 0.24mL |
12.18mL 2.44mL 1.22mL |
24.36mL 4.87mL 2.44mL |
| 参考文献 |
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