Date published: 2026-1-16

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T2R1 Activators

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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Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Isoproterenol Hydrochloride

51-30-9sc-202188
sc-202188A
100 mg
500 mg
$28.00
$38.00
5
(0)

A beta-adrenergic agonist that increases cAMP levels, potentially enhancing T2R1 signaling through G protein activation and downstream effectors.

Forskolin

66575-29-9sc-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
(3)

Directly activates adenylate cyclase, increasing cAMP concentration, which could lead to the stimulation of the T2R1 pathway by promoting G protein-mediated signaling.

IBMX

28822-58-4sc-201188
sc-201188B
sc-201188A
200 mg
500 mg
1 g
$260.00
$350.00
$500.00
34
(1)

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)

37762-06-4sc-201206
sc-201206A
25 mg
100 mg
$105.00
$250.00
8
(2)

A selective inhibitor of phosphodiesterase 5, increases cGMP levels, potentially enhancing T2R1 function by a cGMP-dependent protein kinase pathway.

L-Arginine

74-79-3sc-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
(0)

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

58-08-2sc-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
(1)

As a competitive inhibitor of phosphodiesterases, caffeine elevates intracellular cAMP, possibly enhancing T2R1 signaling via prolonged protein kinase A activation.

Chloroquine

54-05-7sc-507304
250 mg
$69.00
2
(0)

Known to interact with bitter taste receptors, may enhance T2R1 signaling through structural interaction and receptor conformational changes.

Denatonium benzoate

3734-33-6sc-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
(1)

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

130-95-0sc-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
(0)

A bitter compound that can directly activate T2R1 by binding to the receptor, initiating the G protein signaling cascade.

Saccharin

81-07-2sc-212902
sc-212902A
sc-212902B
100 mg
1 g
10 g
$173.00
$235.00
$286.00
(0)

An artificial sweetener that can bind to T2R1, potentially initiating G protein signaling through receptor activation.