Activators & Inhibitors

AZ-GHS-22 (Legacy Tebubio ref. 282T37412). AZ-GHS-22 is an inverse agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor.1It binds to GHS-R1a with an IC50value of 0.77 nM. AZ-GHS-22 decreases food intake in mice by 54% in the first two hours after administration of a 100 mg/kg dose.

Calcitonin (salmon) (trifluoroacetate salt) (Legacy Tebubio ref. 282T37413). Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and 0.317 nM alone and with RAMP1, 2, or 3, respectively. It induces cAMP accumulation in COS-7 cells transfected with CTR2 (EC50 = 0.166 nM). Salmon calcitonin inhibits bone resorption by osteoclasts in a pit formation assay using rat bone slices (ID50 = 0.003 pg/mL) and lowers calcium level in vivo in a bioassay of hypocalcemia in rats (ED15 = 33.9 mg/kg). Formulations containing salmon calcitonin have been used to treat

CAY10771 (Legacy Tebubio ref. 282T37414). CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM.

Tauro-α-muricholic Acid (sodium salt) (Legacy Tebubio ref. 282T37416). Tauro-α-muricholic acid (TαMCA) is an antagonist of the farnesoid X receptor (FXR; IC50 = 28 μM) and a taurine-conjugated form of the murine-specific primary bile acid α-muricholic acid . TαMCA is common in rodents but has also been found in small amounts in human serum.

Z-LLE-AMC (Legacy Tebubio ref. 282T37417). Z-LLE-AMC is a fluorogenic substrate for the caspase-like post-glutamate peptide hydrolase of the 26S proteasome or 20S proteolytic core. Caspase-like activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. Z-LLE-AMC is typically used in cell lysates after experimental treatment.

Z-LLL-AMC (Legacy Tebubio ref. 282T37418). Z-LLL-AMC is a fluorogenic substrate for the chymotrypsin-like activity of the 26S proteasome or 20S proteolytic core. Chymotrypsin-like activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. Z-LLL-AMC is typically used in cell lysates after experimental treatment.

Zetomipzomib (Legacy Tebubio ref. 282T37419). KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2].

3-Methylcatechol (Legacy Tebubio ref. 282T3742). 3-Methylcatechol (2,3-Toluenediol) is an active biochemical.

Ac-ANW-AMC (Legacy Tebubio ref. 282T37420). Ac-ANW-AMC is a fluorogenic substrate for the β5i/LMP7 subunit of the 20S immunoproteasome. [1] Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released, and its fluorescence quantifies the activity of the β5i/LMP7 subunit. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.