Activators & Inhibitors

Amyloid-β (1-42) Peptide (trifluoroacetate salt) (Legacy Tebubio ref. 282T37367). Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-amino acid protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease.1,2,3Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers.1Aβ42 accumulates in the brain of many transgenic mouse models of Alzheimer's disease and, in many models, the onset of amyloid deposition positively correlates with deficits in spatial learning and memory.4

3-(2,4-Dihydroxyphenyl)propanoic acid (Legacy Tebubio ref. 282T3737). 3-(2,4-Dihydroxyphenyl)propanoic acid (Hydroumbellic acid) is a predicted metabolite generated by BioTransformer1 from the metabolism of 3-(2,4-dihydroxyphenyl)prop-2-enoic acid. It is produced by the abkar1 enzyme via a reduction-of-alpha-beta-unsaturated-compounds-pattern1 reaction in human gut microbiota.

Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt) (Legacy Tebubio ref. 282T37370). Amyloid-β (25-35) (Aβ (25-35)) is an 11-residue fragment of the Aβ protein that retains the physical and biological characteristics of the full length peptide. It forms fibrils that react to thioflavin T and Congo red and are organized in a cross-β arrangement of β-strands similar to Aβ (1-40) and Aβ (1-42) fibrils. Aggregated Aβ (25-35) decreases the viability of rat adrenal PC12 cells. It also decreases the viability of primary rat cortical neurons at concentrations ranging from 1 nM to 30 μM.

4(Z),7(Z),10(Z),13(Z),16(Z)-Nonadecapentaenoic Acid (Legacy Tebubio ref. 282T37371). 4(Z),7(Z),10(Z),13(Z),16(Z)-Nonadecapentaenoic acid is an unusual polyunsaturated fatty acid (PUFA) generated during the synthesis of docosahexaenoic acid-d5 . While the physiological properties of this compound are not known, dietary intake of n-3 long-chain PUFAs provides potential health benefits.

4,4-Diphenylbutylamine hydrochloride (Legacy Tebubio ref. 282T37372). 4,4-Diphenylbutylamine exhibits affinity for the 5-HT2A and H1 receptors with Ki values of 2589 and 1670 nM, respectively[1].

4-hydroxy-3-Methoxyphenylglycol (piperazine salt) (Legacy Tebubio ref. 282T37373). 4-hydroxy-3-Methoxyphenylglycol (piperazine salt) is a metabolite of norepinephrine derived in part by deamination of normetanephrine or by O-methylation of dihydroxyphenylglycol after cellular uptake of either intermediate. It is released into the blood and cerebrospinal fluid and has been used as a biochemical index of recent sympathetic nervous system activity.

URB754 (Legacy Tebubio ref. 282T37374). URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

Uridine-3'-monophosphate (sodium salt) (Legacy Tebubio ref. 282T37375). Uridine-3'-monophosphate is a nucleoside used in the biochemical synthesis of ribothymidine-3'-phosphate. It has been used as a bioavailable source of uridine in research studies designed to enhance learning and memory.

PHY34 (Legacy Tebubio ref. 282T37376). PHY34 is a late stage autophagy inhibitor with nanomolar level inhibitory effect and anti-tumor activity against high-grade serous ovarian cancer (HGSOC) in vivo.