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抑制剂/激动剂
细胞生物学
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类器官培养添加剂 cAMP
/ Forskolin/毛喉素

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

货号：A226193 同义名： 佛司可林 / Coleonol; Colforsin

Forskolin是一种腺苷酸环化酶激活剂，能够提高细胞内cAMP水平，并激活PXR与FXR，常用于研究细胞生理学及诱导自噬。其IC50为41 nM，EC50为0.5 μM。Forskolin增强大鼠海马神经前体细胞的神经分化。

Forskolin/毛喉素 化学结构 CAS号：66575-29-9
Forskolin/毛喉素 化学结构
CAS号：66575-29-9
Forskolin/毛喉素 3D分子结构
CAS号：66575-29-9
Forskolin/毛喉素 化学结构 CAS号：66575-29-9
Forskolin/毛喉素 3D分子结构 CAS号：66575-29-9
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Forskolin/毛喉素 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

 		98%
SQ22536 ✔ 99%+
ESI-09 ++

EPAC1, IC50: 3.2 μM

 		+++

EPAC2, IC50: 1.4 μM

 		98%
HJC0350 +++

EPAC2, IC50: 0.3 μM

 		99%
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/毛喉素 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/毛喉素 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293A cells 1–10 μM 1 h To assess the inhibitory effect of Forskolin on mTORC1 activity Elife. 2019 May 21;8:e43038.
MEF cells 10 μM 1 h To assess the inhibitory effect of Forskolin on mTORC1 activity Elife. 2019 May 21;8:e43038.
HEK293T cells 30 μM 30 min Enhanced the interaction between DAGLα and ankyrin-G Biol Psychiatry. 2021 Aug 15;90(4):263-274.
GLUTag cells 10 μM 15 min and 30 min Measure cAMP concentration and PKA activity Gut Microbes. 2021 Jan-Dec;13(1):1987782.
WT cells 10 µM 48 h To investigate the effect of Forskolin on cell respiration and ATP synthesis, results showed that Forskolin increased cell respiration and ATP synthesis. EMBO Mol Med. 2009 Nov;1(8-9):392-406.
CHO-K1 cells 20 µM 30 min Activate PKA to study its effect on KCTD12-induced K+ current desensitization. Results showed that PKA activation significantly slowed KCTD12-induced fast desensitization. Biochem Pharmacol. 2014 Oct 1;91(3):369-79.
Hippocampal neurons 20 µM 30 min Activate PKA to study its effect on KCTD12-induced K+ current desensitization. Results showed that PKA activation significantly slowed KCTD12-induced fast desensitization. Biochem Pharmacol. 2014 Oct 1;91(3):369-79.
MIN6 cells 10 μM 30 min To assess cAMP production, results showed that forskolin-stimulated cAMP production was significantly reduced in Npas4-overexpressing MIN6 cells Diabetes. 2013 Aug;62(8):2808-20.
ScN2a-cl3 cells 1 μM 7 days To evaluate the effect of Forskolin on PrPSc levels in differentiated cells. Results showed that Forskolin did not lead to a rebound in PrPSc levels. PLoS Pathog. 2009 Nov;5(11):e1000673.
Primary cortical neurons 30 μM 30 min Increased the interaction between DAGLα and ankyrin-G and regulated dendritic spine morphology Biol Psychiatry. 2021 Aug 15;90(4):263-274.
SKOV3 cells 20 μM 30 to 40 min Induced endogenous EPAC1 nuclear oligomer formation Nat Commun. 2023 Sep 8;14(1):5521
HUVEC cells 20 μM 30 to 40 min Induced endogenous EPAC1 nuclear oligomer formation Nat Commun. 2023 Sep 8;14(1):5521
HEK cells 20 μM 30 to 40 min Induced EPAC1-YFP nuclear oligomer formation Nat Commun. 2023 Sep 8;14(1):5521

Forskolin/毛喉素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice PSNL and CFA models Oral 2 mg/kg Once daily for 14–33 days Forskolin reversed the PSNL- or CFA-induced decrease in PKA and CREB phosphorylation and BDNF expression, and partially reversed mechanical hypersensitivity and depression-like behaviors Int J Neuropsychopharmacol. 2024 Oct 1;27(10):pyae040
Mice Not specified Intraperitoneal injection 1 mg/kg Single dose, lasting 30 minutes Enhance endothelial cell barrier function, reduce permeability and immune complex deposition J Exp Med. 2004 Oct 4;200(7):835-46
Mice WT and AnkG cKO mice Intraperitoneal injection 0.2 mg/kg Single injection, behavioral tests conducted 30 minutes after injection Evaluated the effect of forskolin on depression- and anxiety-related behaviors, finding that forskolin could not reverse depression-related behavior in AnkG cKO mice but could reverse anxiety-related behavior Biol Psychiatry. 2021 Aug 15;90(4):263-274.

Forskolin/毛喉素 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/毛喉素 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/毛喉素 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/毛喉素 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/毛喉素 技术信息

CAS号66575-29-9
分子式C22H34O7
分子量 410.5
SMILES Code CC(=O)O[C@H]1[C@H]([C@@H]2[C@]([C@H](CCC2(C)C)O)([C@@]3([C@@]1(O[C@@](CC3=O)(C)C=C)C)O)C)O
MDL No. MFCD00082317
别名 佛司可林 ;Coleonol; Colforsin; NSC 375489; NSC 357088; L 75-1362B; HL 362
运输蓝冰
InChI Key OHCQJHSOBUTRHG-KGGHGJDLSA-N
Pubchem ID 47936
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

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

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二

Tags: Forskolin | Coleonol;Colforsin;NSC 375489;NSC 357088;L 75-1362B;HL 362 | 佛司可林 | Organoid Culture Additive | cAMP | AmBeed-信号通路专用抑制剂 | Forskolin/毛喉素 纯度/质量文件 | Forskolin/毛喉素 亚型比较 | Forskolin/毛喉素 生物活性 | Forskolin/毛喉素 动物研究 | Forskolin/毛喉素 临床数据 | Forskolin/毛喉素 参考文献 | Forskolin/毛喉素 实验方案 | Forskolin/毛喉素 技术信息

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