target/Sodium_Channel/8

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt) is a long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase（PKA）, but resistant to degradation by cyclic AMP phosphodiesterase.

HOIPIN-8 sodium is a potent linear ubiquitin chain assembly complex (LUBAC) inhibitor for the study of inflammatory and immune diseases.

Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]

Sodium Channel Inhibitor 4 is a compound that functions as a sodium channel inhibitor [1].

8-Bromo NAD+ serves as a prodrug for the cyclic ADP-ribose (cADPR) inhibitor, 8-bromo cADPR, undergoing conversion to its active form by the enzyme CD38. At a concentration of 1 mM, it effectively inhibits the rise in intracellular calcium levels and chemotaxis triggered by N-formyl-Met-Leu-Phe (fMLP) in mouse bone marrow-derived neutrophils. Furthermore, when applied at 100 µM, this compound reduces LPS-induced nitrite production and decreases the secretion of TNF-α and IL-2 in mouse primary microglial cells.

Sodium Channel inhibitor 2 is a blocker of sodium channel.

8-Chloroadenosine-5’-triphosphate (8-chloro ATP), a potent metabolite of the anticancer agent 8-chloro cyclic AMP (cAMP) and a nucleotide derivative, is produced through the biotransformation of 8-chloro cAMP into 8-chloroadenosine, followed by mono- and diphosphate intermediates. Accumulating for up to 12 hours after the administration of 8-chloro cAMP or 8-chloroadenosine, 8-chloro ATP inhibits cell growth, diminishes endogenous ATP levels, and reduces RNA synthesis without affecting DNA synthesis in multiple myeloma cells derived from patients. Moreover, it obstructs topoisomerase II-α-mediated relaxation of supercoiled pUC19 DNA at concentrations ranging from 1.5 to 8 mM and decreases topoisomerase II-α-enhanced ATP hydrolysis by 50% at a concentration of 1 mM in K562 human myelocytic leukemia cells.

D-Fructose-1,6-bisphosphate sodium salt hydrate is the intermediate in carbohydrate metabolism, including glycolysis and gluconeogenesis. During glycolysis, it is produced by phosphorylation of fructose-6-phosphate by phosphofructokinase. The reverse reaction mediated by fructose-1, 6-diphosphatase-1 is one of the rate-limiting steps of gluconeogenesis. The same reaction occurs in the chloroplasts of plants, D-Fructose-1,6-bisphosphate sodium salt hydrate as part of the reducing pentose phosphate cycle. Since cancer cells use glycolysis as a primary source of metabolic energy production, this pathway has become a major target for cancer chemotherapy.

Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP. It acts as an antagonist of cAMP-dependent protein kinases (PKAs) and is resistant to hydrolysis by cyclic nucleotide phosphodiesterases. Rp-8-bromo-cAMPS more effectively antagonizes cAMP-dependent activation of purified PKA type I from rabbit muscle than PKA type II from bovine heart.

8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac). These Epac proteins are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2].

Cyclic ADP-ribose (cADP-ribose) is a calcium mobilizing nucleotide that is biosynthesized from NAD+ by cADP-ribose synthases, including CD38. cADP-Ribose appears to activate calcium channels in intracellular membranes, which in turn activate ryanodine receptors. 8-bromo-cADP-Ribose is a stable, cell-permeable analog that blocks calcium release evoked by cADP-ribose in sea urchin egg homogenates with an IC50 value of 1.7 μM. It is commonly used to investigate intracellular signaling through cADP-ribose in isolated cells and tissues.

8-Bromoguanosine-5'-O-triphosphate, a derivative of guanosine 5'-triphosphate (GTP) - the energy substrate for protein synthesis and gluconeogenesis, acts as an inhibitor of the E. coli GTPase FtsZ with an inhibition constant (Ki) of 31.8 µM. Furthermore, at a concentration of 500 µM, it facilitates the assembly of porcine brain microtubules in a cell-free assay.

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium functions dually as a selective activator of cyclic AMP-dependent protein kinase (PKA) and as a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA), demonstrating an inhibitory concentration (IC 50) of 0.9 μM. Additionally, this compound inhibits PDE III and PDE IV, while significantly activating Epac, showcasing its diverse pharmacological activities [1] [2].

Sodium Channel inhibitor1 is a novel and selective voltage-gated sodium channel for pain treatment. (IC50 Value of 0.16 uM and 0.41 uM for Na v1.7, V hold-90mV and Na v1.7, V hold-90mV)

D-fructose-1,6-diphosphate (D-fructose-1,6-diphosphate), also known as Fosfructose, is a cytoprotective natural sugar phosphate. It functions by promoting anaerobic glycolysis, which generates adenosine triphosphate (ATP) under ischemic conditions. This compound holds potential for research in cardiovascular ischemia, sickle cell anemia, and asthma.

Esafosfan trisodium (FDP trisodium) is a cytoprotective natural sugar phosphate for the potential treatment of sickle cell anemia, cardiovascular ischemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.