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Forskolinadenylate cyclase activator

Forskolin

Catalog No. B1421
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
25mg $70.00 In stock
50mg $105.00 In stock
100mg $150.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Forskolin

Protocol

Cell experiment [1, 2]:

Cell lines

Human mesenchymal stem cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.075-0.2 mM for 4 days or 7 days; or 10 μM

Applications

Forskolin concentration-dependently decreased human mesenchymal stem cells proliferation after 4 days. Moreover, Forskolin increased alkaline phosphatase (ALP) expression of human mesenchymal stem cells in a dose-dependent manner. Additionally, Forskolin (10 μM) significantly stimulated both vasopressin and oxytocin release from the rat hypothalamo-neurohypophysial (H-NH) system.

Animal experiment [1]:

Animal models

Particles were implanted in subcutaneous pockets of nude male mice model

Dosage form

0.10 or 0.15mM Forskolin

Applications

Treatment with 0.10 mM Forskolin enhanced bone formation by human mesenchymal stromal cells in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Doorn, J., Siddappa, R., van Blitterswijk, C. A. and de Boer, J. (2012) Forskolin enhances in vivo bone formation by human mesenchymal stromal cells. Tissue Eng Part A. 18, 558-567

2. Roszczyk, M. and Juszczak, M. (2014) Forskolin-stimulated vasopressin and oxytocin release from the rat hypothalamo-neurohypophysial system in vitro is inhibited by melatonin. Endokrynol Pol. 65, 125-131

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Chemical Properties

Cas No. 66575-29-9 SDF Download SDF
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
Canonical SMILES CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O
Formula C22H34O7 M.Wt 410.5
Solubility >20.5mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Forskolin is a cell-permeable activator of adenylyl cyclase [1].

Adenylate cyclase is an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to 3',5'-cyclic AMP (cAMP) and pyrophosphate.

Forskolin is a cell-permeable activator of adenylyl cyclase. In rat cerebral cortical membranes, forskolin reversibly and rapidly activated adenylate cyclase with EC50 value of 5-10 μM. GTP and GDP increased the responses to forskolin. In rat cerebral cortical slices, forskolin rapidly increased cAMP by 35-fold with IC50 values of 25 μM [1]. Forskolin inhibited the inactivation of adenylate cyclases induced by N-ethylmaleimide with Kd values of 7.6 and 6.3 μM for the platelet and brain adenylate cyclases, respectively. Also, forskolin protected adenylate cyclases against thermal inactivation. Forskolin activated the platelet adenylate cyclase with IC50 and Kd values of 3-10 μM and 9-11 μM, respectively [2]. In pig epidermal cells, forskolin activated epidermal adenylate cyclase with Ka value of 2-3×10-5 M and induced cAMP accumulations, which then inhibited mitotic in a dose-dependent way [3].

References:
[1].  Seamon KB, Padgett W, Daly JW. Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells. Proc Natl Acad Sci U S A, 1981, 78(6): 3363-3367.
[2].  Awad JA, Johnson RA, Jakobs KH, 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, 258(5): 2960-2965.
[3].  Takeda J, Adachi K, Halprin KM, et al. Forskolin activates adenylate cyclase activity and inhibits mitosis in in vitro in pig epidermis. J Invest Dermatol, 1983, 81(3): 236-240.