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> Forskolin [66575-29-9]

Forskolin [66575-29-9]

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Cat# HY-15371-10mg

Size : 10mg

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Forskoline (Coleonol) est un activateur puissant de adénylate cyclase avec un IC50 de 41 nM et un EC50 de 0,5 μM pour l'adenylyl cyclase de type I. Forskoline est également un inducteur de la formation de AMPc intracellulaire. Forskoline induit la différenciation de divers types de cellules et active les récepteurs du prégnane X (PXR) et FXR. Forskoline exerce un effet inotrope sur le cœur et a des actions antiagrégantes et antihypertensives plaquettaires. Forskoline induit également l'autophagie.

Forskolin (Coleonol) ist ein potenter adenylate cyclase-Aktivator mit einer IC50 von 41 nM und einer EC50 von 0,5 μM für type I adenylyl cyclase. Forskolin ist auch ein Induktor der intrazellulären cAMP-Bildung. Forskolin induziert die Differenzierung verschiedener Zelltypen und aktiviert den pregnane X receptor (PXR) und FXR. Forskolin übt eine inotrope Wirkung auf das Herz aus und hat antiaggregationshemmende und blutdrucksenkende Wirkung auf Blutplättchen. Forskolin induziert auch autophagy.

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.

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Forskolin Chemical Structure

CAS No. : 66575-29-9

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Forskolin Related Antibodies

WB
    U0126 enhances the negative effect of Fsk-IBMX on the development of glioma stem cells (GSCs).
    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 (FSK) -stimulated dephsphorylation of HDAC5 is also inhibited by Thapsigargin (THA) treatment in primary hepatocytes.

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    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.

    IC50: 41 nM (Adenylyl cyclase)
    EC50: 0.5 μM (Adenylyl cyclase)
    In Vitro

    Forskolin (Coleonol) is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells.
    Forskolin (Fsk) is a naturally occurring diterpene isolated from Coleus forskholii, directly activates adenylyl cyclase (AC) through its catalytic subunit to increase intracellular levels of cyclic adenosine monophosphate (cAMP).
    Forskolin (Fsk) affects the proliferation of the human T-cell lines such as Kit 225 and MT-2. Forskolin treatment inhibits the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner with an IC50 equal to ~5 μM Fsk. Forskolin treatment (10-100 μM) increases cAMPi levels ~5- to 20-fold above basal levels, which reache maximum levels between 50-100 μM Forskolin.

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

    Forskolin Related Antibodies
    In Vivo

    The Forskolin (Coleonol)-treated Mrp4-/- mice shows an increased number of Ki67-positive and cleaved caspase 3-positive ECs, a significant decrease in the amount of pericyte coverage, and a reduced number of empty sleeves. In pups exposed to hyperoxia (75% oxygen) from P7 to P12, the Mrp4-/- mice shows a significant increase in the unvascularized retinal area.
    The average blood glucose in the healthy rat group is 102.12±1.94 mg/dL, 101.25±3.56 for control group and 103±2.08 in forskolin group. The data shows that glucose levels at the end of the study are lower in forskolin group, with a significant difference according to the statistical tests applied (p=0.03).

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

    410.50

    C22H34O7

    66575-29-9

    Solid

    White to off-white

    O=C1[C@@]2(O)[C@]([C@@H](OC(C)=O)[C@@H](O)[C@@]3(02)C(C)(C)CC[C@H](O)[C@@]32C)(C)O[C@@](C)(C=C)C1
    • Terpenoids
    • Diterpenoids
    • Plants
    • Compositae
    • Gochnatia polymorpha (Less) Cabr.
    • Plants
    • Labiatae

    Room temperature in continental US; may vary elsewhere.

    4°C, protect from light

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

    In Vitro: 

    DMSO : 100 mg/mL (243.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2436 mL 1.2180 mL 2.4361 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo:

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    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
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    • [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.  [Content Brief]

      [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.  [Content Brief]

      [3]. Mayati A, et al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

    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.

    MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

    Mice
    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
    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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

    • [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.  [Content Brief]

      [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.  [Content Brief]

      [3]. Mayati A, et al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

    • [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.

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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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    • Stem Cell/Wnt GPCR/G Protein Metabolic Enzyme/Protease Autophagy Epigenetics TGF-beta/Smad
    • Organoid Adenylate Cyclase FXR Autophagy PKC
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    Keywords:

    Forskolin66575-29-9Coleonol Colforsin HL 362HL362HL 362HL-362OrganoidAdenylate CyclaseFXRAutophagyPKCAdenylyl cyclaseNR1H4Protein kinase CcAMPpregnaneX receptorPXRnotropicantiaggregatoryantihypertensiveexosomeprostatecancerInhibitorinhibitorinhibit

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