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Forskolin [66575-29-9]

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Cat# HY-15371-10mg

Size : 10mg

Brand : MedChemExpress

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Description

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]

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]

In Vitro

Forskolin (Coleonol) is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells^[8].
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)^[1].
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^[6].

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

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^[2].
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)^[7].

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

Molecular Weight

410.50

Formula

C₂₂H₃₄O₇

CAS No.

66575-29-9

Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@@]2(O)[C@]([C@@H](OC(C)=O)[C@@H](O)[C@@]3(01)C(C)(C)CC[C@H](O)[C@@]32C)(C)O[C@@](C)(C=C)C1

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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.

Purity & Documentation

Purity: 99.78%

Data Sheet (293 KB) SDS (393 KB)

COA (265 KB) HNMR (273 KB) LCMS (96 KB) Elemental Analysis Report (122 KB)

Handling Instructions (2659 KB)

References

[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]

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Forskolin [66575-29-9]

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