Results for Activators & Inhibitors ( 70875 )
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Cyclic ADP-Ribose (ammonium salt) (Legacy Tebubio ref. 282T37475). Cyclic ADP-ribose (cADP-ribose) is an endogenous metabolite of NAD+ that mobilizes the release of stored Ca2+ in the endoplasmic reticulum via ryanodine receptors in various cell types.[1],[2],[3],[4],[5] This second messenger is generated via the cADP-ribose synthases CD38 and CD157.[6],[5],[7] cADP-Ribose may also trigger the cell surface Ca2+ influx channel TRPM2 in a temperature-dependent manner.[8]
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L-858,051 (hydrochloride) (Legacy Tebubio ref. 282T37477). 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.
Acetyl β-Endorphin (1-26) (human) (trifluoroacetate salt) (Legacy Tebubio ref. 282T37478). Acetyl β-endorphin (1-26) is a neuropeptide found in rat hippocampus, brain stem, and pituitary. It is also present in the human hypothalamus, where it comprises approximately 4.9% of total β-endorphin peptides. Acetyl β-endorphin (1-26) is produced through posttranslational processing of β-endorphin and is processed similarly in rat and human hypothalamus. Levels of acetyl β-endorphin (1-26) increase in the rat pars intermedia and brain stem following chronic administration of haloperidol .
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Diclofenac methyl ester (Legacy Tebubio ref. 282T37482). Diclofenac methyl ester is a hydrophobic prodrug form of diclofenac which is a non-steroidal anti-inflammatory drug (NSAID). Diclofenac methyl ester is more soluble than diclofenac acid in isopropylmyristate but with higher toxicity.
Difelikefalin (trifluoroacetate salt) (Legacy Tebubio ref. 282T37483). Difelikefalin is a κ-opioid receptor (KOR) agonist.1It activates KOR in HEK293 cells expressing the human receptor (EC50= 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50= 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor (MOR; EC50= >1 μM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).
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1-Salicylate Glucuronide (Legacy Tebubio ref. 282T37484). 1-Salicylate glucuronide is a metabolite of salicylic acid and aspirin .1It is formed from salicylic acid primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A9 but also by a variety of other UGT isoforms and from aspirinviasalicylic acid as an intermediate.