Activators & Inhibitors

Phospho-L-Arginine (lithium salt hydrate) (Legacy Tebubio ref. 282T37802). Phospho-L-arginine is a phosphorylated form of L-arginine and a highly diffusible, high-energy metabolite and phosphagen involved in energy storage in invertebrates including crustaceans, insects, and Trypanosoma species. In the locust L. migratoria, phospho-L-arginine is found in the flight muscles, where it acts as both a buffer system and shuttle mechanism for high-energy phosphate. Measurement of phospho-L-arginine by 31P-NMR spectroscopy has been used to study invertebrate energy metabolism in vivo.

8-bromo-Cyclic ADP-Ribose (sodium salt) (Legacy Tebubio ref. 282T37803). 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.

8MDP (Legacy Tebubio ref. 282T37804). Potent equilibrative nucleoside transporter 1 (ENT1) inhibitor (IC50 = 0.43 nM). Inhibits hENT1 and hENT2 uptake of [H3]uridine in K562 cells and K15NTD cells respectively.

JNJ-55308942 (Legacy Tebubio ref. 282T37806). JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.

JTV-519 fumarate (Legacy Tebubio ref. 282T37807). JTV-519 fumarate (K201 fumarate) is a SERCA blocker and partial agonist at the ryanodine receptor with antiarrhythmic and cardioprotective effects, improves sarcoplasmic reticulum calcium leakage, and may be useful in the study of anxiety disorders.

Kaliotoxin (Legacy Tebubio ref. 282T37808). Kaliotoxin is an inhibitor of neuronal BK-type peptide groups and specifically inhibits Kv channels and calcium-activated potassium channels. Kaliotoxin has research significance on the regulation of cell membrane potential and neuronal excitability. The product number is T37808 and the CAS number is 145199-73-1

Alphitonin (Legacy Tebubio ref. 282T37809). Alphitonin is a flavonoid that has been found in L. leptolepis wood.1 It is also a metabolic intermediate that is formed during the catabolism of quercetin by the human gut bacteria E. ramulus.2,3

Jujuboside B (Legacy Tebubio ref. 282T3781). Jujuboside B has potent inhibitory effects on collagen-, thrombin-, AA-, and ADP-induced aggregation, and also exhibits superior protection on the thromboembolic model.

6',7'-Epoxybergamottin (Legacy Tebubio ref. 282T37810). 6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.