Activators & Inhibitors

True Blue (Legacy Tebubio ref. 282T37667). True blue is a fluorescent neuronal retrograde tracer that labels the nucleus, nucleolus, cell body, proximal dendrites, and axons of neurons. It displays excitation/emission maxima of 373/404 nm, respectively.

CAY10448 (Legacy Tebubio ref. 282T37668). Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel, the vanilloid receptor 1 (VR1), or transient receptor potential vanilloid 1 (TRPV1). CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of approximately 10 nM.

CAY10498 (Legacy Tebubio ref. 282T37669). The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated.

Polygalacic acid (Legacy Tebubio ref. 282T3767). Polygalacic acid (Virgaureagenin G) is a triterpenoid isolated from the root of Polygala tenuifolia Willd that inhibits MMP expression. Polygalacic acid (Virgaureagenin G) can significantly improve the responsiveness of the cholinergic system, such as decreased acetylcholinesterase (AChE) activity, increased choline acetyltransferase (ChAT) activity, and increased acetylcholine (ACh) levels in the hippocampus and frontal cortex. Polygalacic acid (Virgaureagenin G) can also inhibit IL-1β-induced Wnt/β-catenin activation and mitogen-activated protein kinase (MAPK) signaling pathways in chondrocytes, and is used in osteoarthritis (OA) related research.

CAY10568 (Legacy Tebubio ref. 282T37670). Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported. CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.

CAY10608 (Legacy Tebubio ref. 282T37671). N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.

Aspartocin D (Legacy Tebubio ref. 282T37672). Aspartocin D can be obtained from the fermentation broth of Streptomyces canus strain FIM0916.

Asperlactone (Legacy Tebubio ref. 282T37673). Asperlactone is a nematicidal, insecticidal, antibacterial, and antifungal polyketide metabolite produced from A. westerdijkiae.

Aspyrone (Legacy Tebubio ref. 282T37674). Aspyrone is a polyketide fungal metabolite found in [Aspergillus] with diverse biological activities. It is active against 13 fungi at 20 μg/ml and 21 bacteria at 100 μg per disc. Aspyrone (10-1,000 mg/L) is nematocidal against [P. penetrans].