Forskolin (Coleonol; Colforsin)

Alias:
Cat No.:V1481 Purity: ≥98%
Forskolin (HL-362; L-75-1362B; NSC-357088; NSC-375489; Coleonol; Colforsin), a naturally occurring and cell-permeable diterpene extracted from the Indian Coleus plant (C. forskohlii), is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types.
Forskolin (Coleonol; Colforsin) Chemical Structure CAS No.: 66575-29-9
Product category: cAMP
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Forskolin (HL-362; L-75-1362B; NSC-357088; NSC-375489; Coleonol; Colforsin), a naturally occurring and cell-permeable diterpene extracted from the Indian Coleus plant (C. forskohlii), is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types. It can improve the in vivo production of bone by human mesenchymal stromal cells. In the study and investigation of cell physiology, forskolin is frequently used to increase cAMP levels. With an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase, respectively, it functions as a strong activator of adenylate cyclase. In the rat myometrium, forskolin regulates the production of cyclic AMP. Interactions with isoproterenol and prostaglandins E2 and I2.

Biological Activity I Assay Protocols (From Reference)
Targets
Adenylyl cyclase ( IC50 = 41 nM ); Adenylyl cyclase ( EC50 = 0.5 μM )
ln Vitro

In vitro activity: Forskolin increases cAMP levels in preparations of membranes, cells, or tissues. In addition to activating AC, forskolin also interacts with ion channels and glucose transporters, among other proteins. With the exception of AC9, which is somewhat less effective than the other nine transmembrane isoforms of AC, forskolin can activate nine of them. This property makes it possible to identify and measure high-affinity binding sites, or G-proteins (Gs)–AC complexes. Forskolin-stimulated cAMP generation in cells is facilitated by GPCR-mediated s activation because s-Forskolin potentiates AC activity.[1] Forskolin stimulates adenylate cyclase activity without interacting with cell surface receptors. The potentiation of cAMP by forskolin consequently suppresses the release of histamine and the degranulation of mast cells and basophils, reduces intraocular pressure and blood pressure, stops platelet aggregation, increases thyroid hormone secretion, vasodilation, bronchodilation, and fat cell lipolysis. Regardless of the production of cAMP, forskolin inhibits the binding of platelet-activating factor (PAF). This effect may be due to forskolin's direct interaction with PAF or to forskolin's interference with PAF's ability to bind to receptor sites. Forskolin suppresses the transport of glucose in erythrocytes, adipocytes, platelets, and other cells. It also seems to have an impact on a number of membrane transport proteins. Forskolin is used to treat with glaucoma. [2]

ln Vivo
Colforsin, also known as Forskolin, HL 362, or Coleonol, is a widely used cAMP-raising agent that ubiquitously activates eukaryotic adenylyl cyclase (AC) in a range of cell types. Additionally, it promotes autophagy and activates FXR and PXR activity. [4]
Cell Assay
In 96-well plates, 5×104 cells of either MT-2 or Quiescent Kit 225 are seeded into each well. Afterwards, cells are pretreated for one hour at concentrations of 1, 5, 10, 25, 50, and 100 μM of forskolin or 1% DMSO (vehicle). Following 20 hours of culture at 37°C and IL-2 stimulation, the cells are harvested. A 20-hour treatment of 1% DMSO is given to control cells. [3H]thymidine is pulsed into the cells at a concentration of 0.5 μCi/200 μL during the last 4 hours of incubation. Using liquid scintillation counting, cells are collected onto fiberglass filters for analysis.
Animal Protocol
Mice: Mice C57BL/6J are employed. established and frequently backcrossed Mrp4-knockout miceto the C57BL/6J mice At postnatal days 4 (P4) and 5, neonatal mice receive an intraperitoneal injection of forskolin (P5). The controls are mice that have been injected with DMSO. After the P6 euthanasia of the treated mice, their retinas are separated for whole-mount immunohistochemistry (IHC). To compare the retinal vascular phenotypes of WT and Mrp4-deficient mice, the optimal concentration of Forskolin was found to be 1.0 μg/50 μL (0.3 mg/kg) at P4 and 1.5 μg/50 μL (0.5 mg/kg) at P5. This was achieved by testing the effects of different Forskolin concentrations on the survival rate and retinal vasculature.
Rats: Four groups of male Wistar rats, ages 10–14 weeks, with mean weights of 300 g±50 g, are created: eight are kept in good health, and 19 are experimentally made to develop diabetes. For eight weeks, either 6 mg/kg of forskolin per day is given orally to both diabetic and healthy rats as a control. Before and after Forskolin treatment, each group's blood glucose levels are measured. After eight weeks of the prescribed treatment and two weeks following the confirmation of diabetes (three weeks following the induction), the diabetic rats are tested.
References

[1]. Cell Mol Neurobiol . 2003 Jun;23(3):305-14.

[2]. J Postgrad Med . 2012 Jul-Sep;58(3):199-202.

[3]. Nucleic Acids Res . 2022 Apr 8;50(6):3323-3347.

[4]. Br J Pharmacol . 2016 Nov;173(22):3248-3260.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H34O7
Molecular Weight
410.5
Exact Mass
410.23
Elemental Analysis
C, 64.37; H, 8.35; O, 27.28
CAS #
66575-29-9
Related CAS #
66575-29-9
Appearance
Solid powder
SMILES
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
InChi Key
OHCQJHSOBUTRHG-KGGHGJDLSA-N
InChi Code
InChI=1S/C22H34O7/c1-8-19(5)11-14(25)22(27)20(6)13(24)9-10-18(3,4)16(20)15(26)17(28-12(2)23)21(22,7)29-19/h8,13,15-17,24,26-27H,1,9-11H2,2-7H3/t13-,15-,16-,17-,19-,20-,21+,22-/m0/s1
Chemical Name
[(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-5-yl] acetate
Synonyms

Coleonol; HL-362; L-75-1362B; NSC-357088; NSC-375489; HL 362; L 75-1362B; NSC 357088; NSC 375489

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 82~100 mg/mL (199.8~243.6 mM)
Water: <1 mg/mL
Ethanol: ~37 mg/mL (~90.1 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01254006 Completed Drug: forskolin, rutin and
vitamins B1 and B2
Glaucoma University of Roma La Sapienza N/A Not Applicable
Biological Data
  • Forskolin treatment decreased histopathological deterioration and hepatic fibrogenesis induced by CCl4. Br J Pharmacol . 2016 Nov;173(22):3248-3260.
  • Forskolin treatment reduced inflammation associated with CCl4‐induced liver fibrosis. Br J Pharmacol . 2016 Nov;173(22):3248-3260.
  • Forskolin treatment suppressed NF‐κB expression in liver tissue. Br J Pharmacol . 2016 Nov;173(22):3248-3260.
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