佛司可林;弗斯可林

Product Name: Forskolin

CAS No.: 66575-29-9

Synonyms: Colforsin; ForsLean; Coleonol; HL 362; L 75-1362B; NSC 357088; NSC 375489; 7β-Acetoxy-8,13-epoxy-1α,6β,9α-trihydroxylabd-14-en-11-one

Chemical Name: (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-(Acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1H-naphtho[2,1-b]pyran-1-one; [3R-(3α,4aβ,5β,6β,6aα,10α,10aβ,10bα)]-5-(Acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1H-naphtho[2,1-b]pyran-1-one; 5-(acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-1H-Naphtho[2,1-b]pyran-1-one

Molecular Formula: C22H34O7

Molecular Weight: 410.50

Appearance: Off-white to white powder

Assay(HPLC)≥98%

Biological Activity: Cell-permeable activator of adenylyl cyclase. Hypotensive and vasodilatory agent. Induces neuronal differentiation in stem cells and in several neuroblastoma. Used to reprogram mouse embryonic fibroblasts to induced pluripotent stem cells in combination with three other small molecules. Activates adenylate cyclase leading to an increase in the intracellular concentration of cAMP.

 Cyclic AMP (cAMP) is an important signal carrier necessary for the proper biological response of cells to hormones, neurotransmitters, and other extracellular signals. Forskolin is a naturally occurring diterpene that is produced by the Indian Coleus plant (C. forskohlii). It directly activates adenylyl cyclase through its catalytic subunit and is commonly used to raise levels of cAMP in a wide variety of intact cells and tissue preparations. Forskolin binds to adenylyl cyclase in membranes from stably transfected Sf9 cells expressing type 1 adenylyl cyclase with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay assessing formation of cAMP from ATP. Forskolin also interacts with glucose transporters and certain ion channels and has been used for examining adenylyl cyclase expression, regulation, and G protein signaling.

 The major cell-permeable diterpene isolated from the Indian plant Coleus forskohlii. At low doses, it acts as a positive inotropic agent. At higher doses, it serves as a hypotensive and vasodilatory agent due to its actions as a smooth muscle relaxant. No major side effects are observed at effective doses. Forskolins pharmacological activities are due to its activation of adenylate cyclase (EC50 = 4 µM), resulting in increased cAMP levels. The exact mechanism of forskolins positive inotropic effect is unknown but may be related to a cAMP-dependent increase in Na+ permeability that results in indirect augmentation of Ca2+ release. Inhibits MAP kinase in rat renal mesangial cells (IC50 = 25 µM). Also acts as a Hh pathway antagonist. Shown to inhibit apoptosis in cerebellar granule cells and to induce apoptosis in resting human B lymphocytes.

 An adenylate cyclase activator and MAP kinase inhibitor. Forskolin is a diterpenoid isolated from Coleus forskohlii, interacts directly with the catalytic subunit of A cyclase (adenylate cyclase), activating the enzyme and raising intracellular levels of cAMP. Forskolin is cell permeable and active in vivo producing positive inotropic, platelet anti-aggregatory and anti-hypertensive effects. Has also been shown to exhibit smooth muscle relaxant activity, decrease in intraocular pressure and the promotion of hormonal release from the pituitary glands. Inhibits MAP kinase, induces phosphorylation of CREB, connexin 43, Bad, ATF-1 and PKB. Forskolin is an inhibitor of AChR.

 Forskolin is a cell permeable diterpenoid isolated from Coleus forskohlii. Cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties. Many of its biological effects are due to its activation of adenylyl cyclase and the resulting increase in intracellular cAMP concentration.Forskolin effects calcium currents and inhibits MAP kinase.