1. Stem Cell/Wnt GPCR/G Protein Metabolic Enzyme/Protease Autophagy TGF-beta/Smad Epigenetics
  2. Organoid Adenylate Cyclase FXR Autophagy PKC
  3. Forskolin

Forskolin  (Synonyms: 毛喉素; Coleonol; Colforsin; HL 362)

目录号: HY-15371 纯度: 98.71%
COA 产品使用指南

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)。

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Forskolin Chemical Structure

Forskolin Chemical Structure

CAS No. : 66575-29-9

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10 mM * 1 mL in DMSO ¥660
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5 mg ¥600
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10 mg ¥810
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50 mg ¥1500
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Customer Review

Other Forms of Forskolin:

MCE 顾客使用本产品发表的 120 篇科研文献

WB

    Forskolin purchased from MCE. Usage Cited in: J Cell Biochem. 2019 Jan;120(1):321-331.  [Abstract]

    U0126 enhances the negative effect of Fsk-IBMX on the development of glioma stem cells (GSCs).

    Forskolin purchased from MCE. Usage Cited in: J Cell Biochem. 2019 Jan;120(1):321-331.  [Abstract]

    The combination of Fsk and IBMX (Fsk-IBMX) inhibits the expression of cAMP related protein. The results of Western blot in glioma stem cells (GSCs).

    Forskolin purchased from MCE. Usage Cited in: J Lipid Res. 2018 Feb;59(2):330-338.  [Abstract]

    Forskolin (FSK) -stimulated dephsphorylation of HDAC5 is also inhibited by Thapsigargin (THA) treatment in primary hepatocytes.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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[1]. Forskolin is also an inducer of intracellular cAMP formation[2]. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR[3]. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy[4][5].

    IC50 & Target

    IC50: 41 nM (Adenylyl cyclase)[1]
    EC50: 0.5 μM (Adenylyl cyclase)[1]

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BT-474 IC50
    > 100 μM
    Compound: 1
    Antiproliferative activity against human BT474 cells after 48 hrs by Alamar blue assay
    Antiproliferative activity against human BT474 cells after 48 hrs by Alamar blue assay
    [PMID: 28838692]
    HEK293 EC50
    0.0937 μM
    Compound: FSK
    Agonist activity at recombinant human AC8 expressed in human HEK293 cells assessed as fold increase in cAMP level by LANCE Ultra cAMP Detection kit method
    Agonist activity at recombinant human AC8 expressed in human HEK293 cells assessed as fold increase in cAMP level by LANCE Ultra cAMP Detection kit method
    [PMID: 31776060]
    HepG2 EC50
    2.7 μM
    Compound: Colforsin
    Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
    Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
    [PMID: 20966043]
    HepG2 EC50
    7.1 μM
    Compound: Colforsin
    Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
    Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
    [PMID: 20966043]
    HepG2 EC50
    7.9 μM
    Compound: Colforsin
    Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
    Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
    [PMID: 20966043]
    MCF7 IC50
    63.3 μM
    Compound: 1
    Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue assay
    [PMID: 28838692]
    Vero CC50
    674 μM
    Compound: 10
    Cytotoxicity against Vero E6 cells by MTT assay
    Cytotoxicity against Vero E6 cells by MTT assay
    [PMID: 17663539]
    Vero EC50
    7.5 μM
    Compound: 10
    Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA
    Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA
    [PMID: 17663539]
    体外研究
    (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]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (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]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    410.50

    Formula

    C22H34O7

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    毛喉素

    结构分类
    初始来源
    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
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (243.61 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4361 mL 12.1803 mL 24.3605 mL
    5 mM 0.4872 mL 2.4361 mL 4.8721 mL
    查看完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    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

    • 方案 一

      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); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      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。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.78%

    参考文献
    Cell Assay
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4361 mL 12.1803 mL 24.3605 mL 60.9013 mL
    5 mM 0.4872 mL 2.4361 mL 4.8721 mL 12.1803 mL
    10 mM 0.2436 mL 1.2180 mL 2.4361 mL 6.0901 mL
    15 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0601 mL
    20 mM 0.1218 mL 0.6090 mL 1.2180 mL 3.0451 mL
    25 mM 0.0974 mL 0.4872 mL 0.9744 mL 2.4361 mL
    30 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
    40 mM 0.0609 mL 0.3045 mL 0.6090 mL 1.5225 mL
    50 mM 0.0487 mL 0.2436 mL 0.4872 mL 1.2180 mL
    60 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
    80 mM 0.0305 mL 0.1523 mL 0.3045 mL 0.7613 mL
    100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6090 mL
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    目录号:
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