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  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)

目錄號: HY-15371 純度: 98.71%
COA 產(chǎn)品使用指南

Forskolin (Coleonol) 是一種有效的腺苷酸環(huán)化酶 (adenylate cyclase) 激活劑,對于 I 型腺苷酸環(huán)化酶,IC50 為 41 nM,EC50 為 0.5 μM。Forskolin 也是一種細胞內(nèi) cAMP 形成的誘導(dǎo)劑。Forskolin 誘導(dǎo)多種細胞類型的分化并激活孕烷 X 受體 (PXR) 和 FXR。Forskolin 對心臟產(chǎn)生正性肌力作用,并具有血小板抗凝集和降壓作用。Forskolin 也可誘導(dǎo)細胞自噬 (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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Customer Review

Other Forms of Forskolin:

MCE 顧客使用本產(chǎn)品發(fā)表的 124 篇科研文獻

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

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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]

    細胞效力
    (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]
    體外研究
    (In Vitro)

    Forskolin (Coleonol) 也是前列腺癌 (PC) 細胞中有效的外泌體生物合成和/或分泌激活劑[8]
    Forskolin (Fsk) 是一種從錦紫蘇中分離的天然二萜 forskholii,通過其催化亞基直接激活腺苷酸環(huán)化酶 (AC),從而增加細胞內(nèi)環(huán)磷酸腺苷 (cAMP) 的水平[1]。
    Forskolin (Fsk) 影響人類 T 細胞系 (如 Kit 225 和 MT-2) 的增殖。Forskolin 處理以劑量依賴性方式抑制 Kit 225 和 MT-2 細胞的增殖,IC50 等于 ~5 μM Fsk。Forskolin 處理 (10-100 μM) 將 cAMPi 水平提高到基礎(chǔ)水平的 5 到 20 倍,達到最大水平 50-100 μM Forskolin[6]。

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

    體內(nèi)研究
    (In Vivo)

    Forskolin (Coleonol) 處理的 Mrp4-/- 小鼠顯示 Ki67 陽性和裂解半胱天冬酶 3 陽性 EC 數(shù)量增加,周細胞覆蓋量顯著減少。在從 P7 到 P12 暴露于高氧 (75% 氧氣) 的幼崽中,Mrp4-/- 小鼠顯示無血管化視網(wǎng)膜區(qū)域顯著增加[2]
    健康大鼠組平均血糖為 102.12±1.94 mg/dL,對照組為 101.25±3.56,F(xiàn)orskolin 組為 103±2.08。數(shù)據(jù)顯示,F(xiàn)orskolin 組在研究結(jié)束時的血糖水平較低,根據(jù)所應(yīng)用的統(tǒng)計檢驗具有顯著差異 (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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    毛喉素

    結(jié)構(gòu)分類
    初始來源
    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    4°C, protect from light

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

    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 100 mg/mL (243.61 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% Corn Oil

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

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

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

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.78%

    參考文獻
    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.

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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    產(chǎn)品名稱:
    Forskolin
    目錄號:
    HY-15371
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