Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor Diterpenoids of Coleus forskohliiPhytochemistry28(3)859-862(1989) 2.Joost, H.G., Habberfield, A.D., Simpson, I.A., et al.Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of actionMol. Pharmacol.33(4)449-453(1988) 3.Bhat, S.V., Dohadwalla, A.N., Bajwa, B.S., et al.The antihypertensive and positive inotropic diterpene forskolin: Effects of structural modifications on its activityJ. Med. Chem.26(4)486-492(1983) 4.McCulloch, A.J., Thomson, T.A., and Deacon, R.Hypoxic amnesia and its reversal with forskolinBiochem. Soc. Trans.17(1)212-213(1988)
L-858,051 is a water-soluble analog of forskolin , a cell-permeant activator of adenylate cyclase. L-858,051 activates adenylate cyclase (EC50 = 3 μM), inhibits glucose transport, and blocks cytochalasin B binding in rat adipocyte membranes. L-858,051 is used to activate adenylate cyclase and initiate signaling through elevated cAMP synthesis in a variety of cell types in culture.
LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM[1]. Ki: 0.29 μM (FABP4), 1.3 μM (FABP3)[1]Kd: 2.05 μM (FABP4)[1] LDN 0088050 significantly inhibits LPS-induced expression of both TNFα and IL-6 in RAW264.7 cells[1]. [1]. Zhou Y, et al. The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation. Bioorg Med Chem. 2016 Sep 15;24(18):4310-4317.
10-Nitrolinoleate is the product of nitration of linoleate by NO-derived reactive species. Other nitrolinoleates detected in human plasma and urine include 9-, 12-, and 13-nitrolinoleate. Nitrolinoleates activate peroxisome proliferator-activated receptor γ (PPARγ; Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake. Nitrolinoleates can also be metabolized by smooth muscle cells to produce nitrite derivatives which in turn form NO, leading to increased cGMP production and smooth muscle relaxation. Through the same mechanism, nitrolinoleate-derived NO suppresses leukocyte adhesion, in part through nitrosation of CD40. Alteratively, nitrolinoleates can act independently of NO/cGMP and PPARγ signaling to suppress neutrophil and macrophage functions.
IQZ23 is a chemical compound that effectively inhibits adipocyte differentiation by activating the AMPK pathway. It demonstrates high efficacy in reducing triglyceride levels (EC50=0.033 μM) in 3T3-L1 adipocytes. Given its properties, IQZ23 holds potential for research related to obesity and metabolic disorders.