T2R1 activators encompass a variety of chemical compounds that engage and enhance the receptor's functional activity through different biochemical mechanisms within its associated signaling pathways. Compounds such as Isoproterenol, Forskolin, and IBMX augment intracellular cAMP levels, a critical second messenger in the G protein-coupled signaling cascade that T2R1 is a part of. The elevation of cAMP by these compounds could potentiate the T2R1 signaling, leading to enhanced bitterness perception. Conversely, Zaprinast and L-Arginine function by elevating cGMP levels, another second messenger that, through cGMP-dependent protein kinases, may enhance T2R1 signaling.
Caffeine, maintaining cAMP levels by inhibiting its breakdown, and Chloroquine, through structural interaction, can also lead to more robust T2R1 signaling. Direct activators like Denatonium Benzoate and Quinine bind to the receptor's ligand-binding domain, initiating a conformational change that triggers the associated G protein signaling pathways. Saccharin, while primarily known as an artificial sweetener, is included for its ability to bind to and potentially activate T2R1, indicating a polypharmacology that can influence multiple taste pathways. Furthermore, Gymnemic Acid and Copper(II) Sulfate represent unique modulators of T2R1 activity. Copper(II) Sulfate may act as an allosteric activator, binding to a site distinct from the ligand-binding domain to modulate the receptor's activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $28.00 $38.00 | 5 | |
A beta-adrenergic agonist that increases cAMP levels, potentially enhancing T2R1 signaling through G protein activation and downstream effectors. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $78.00 $153.00 $740.00 $1413.00 $2091.00 | 73 | |
Directly activates adenylate cyclase, increasing cAMP concentration, which could lead to the stimulation of the T2R1 pathway by promoting G protein-mediated signaling. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $260.00 $350.00 $500.00 | 34 | |
A non-specific inhibitor of phosphodiesterases, leading to an increase in cAMP levels, which could indirectly increase T2R1 signaling by reducing cAMP breakdown. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $105.00 $250.00 | 8 | |
A selective inhibitor of phosphodiesterase 5, increases cGMP levels, potentially enhancing T2R1 function by a cGMP-dependent protein kinase pathway. | ||||||
L-Arginine | 74-79-3 | sc-391657B sc-391657 sc-391657A sc-391657C sc-391657D | 5 g 25 g 100 g 500 g 1 kg | $20.00 $31.00 $61.00 $219.00 $352.00 | 2 | |
A precursor of nitric oxide, which may enhance T2R1 activity through cGMP pathway modulation after its conversion to nitric oxide by nitric oxide synthase. | ||||||
Caffeine | 58-08-2 | sc-202514 sc-202514A sc-202514B sc-202514C sc-202514D | 50 g 100 g 250 g 1 kg 5 kg | $33.00 $67.00 $97.00 $192.00 $775.00 | 13 | |
As a competitive inhibitor of phosphodiesterases, caffeine elevates intracellular cAMP, possibly enhancing T2R1 signaling via prolonged protein kinase A activation. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $69.00 | 2 | |
Known to interact with bitter taste receptors, may enhance T2R1 signaling through structural interaction and receptor conformational changes. | ||||||
Denatonium benzoate | 3734-33-6 | sc-234525 sc-234525A sc-234525B sc-234525C sc-234525D | 1 g 5 g 25 g 100 g 250 g | $32.00 $47.00 $141.00 $473.00 $921.00 | ||
Recognized as one of the most bitter substances, likely to activate T2R1 directly by binding to the receptor site and causing a conformational change that activates the G protein. | ||||||
Quinine | 130-95-0 | sc-212616 sc-212616A sc-212616B sc-212616C sc-212616D | 1 g 5 g 10 g 25 g 50 g | $79.00 $104.00 $166.00 $354.00 $572.00 | 1 | |
A bitter compound that can directly activate T2R1 by binding to the receptor, initiating the G protein signaling cascade. | ||||||
Saccharin | 81-07-2 | sc-212902 sc-212902A sc-212902B | 100 mg 1 g 10 g | $173.00 $235.00 $286.00 | ||
An artificial sweetener that can bind to T2R1, potentially initiating G protein signaling through receptor activation. | ||||||