Date published: 2025-12-24

1-800-457-3801

SCBT Portrait Logo
Seach Input

T2R4 Inhibitors

T2R4 inhibitors pertain to a class of chemical compounds that specifically antagonize or inhibit the action of the T2R4 receptor, which is one of the numerous bitter taste receptors classified within the Type 2 taste receptor family (T2R). The T2R family is a subset of the G protein-coupled receptor (GPCR) superfamily, known for its role in detecting bitter compounds. T2R4, like other T2R receptors, is expressed on the surface of taste receptor cells located within the taste buds of the tongue and is responsible for the transduction of bitter taste stimuli. When a bitter substance binds to T2R4, it activates a signal transduction pathway that ultimately leads to the perception of bitterness. The function and structure of T2R4 receptors are complex and highly specialized. These receptors consist of a seven-transmembrane domain structure typical of GPCRs, allowing them to traverse the cell membrane seven times. This structure is crucial for the receptor's ability to interact with bitter molecules and initiate a cascade of intracellular events. T2R4 inhibitors, therefore, are designed to fit into the binding site of the receptor, preventing activation by bitter substances. By blocking this interaction, these inhibitors can modulate the signal transduction pathway that normally leads to the sensation of bitterness. The design of T2R4 inhibitors often involves detailed knowledge of the receptor's binding pocket, which can be elucidated through various methods such as X-ray crystallography or computational modeling, providing insights into the spatial arrangement of atoms within the receptor and enabling the design of molecules that can effectively prevent receptor activation.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Denatonium benzoate

3734-33-6sc-234525
sc-234525A
sc-234525B
sc-234525C
sc-234525D
1 g
5 g
25 g
100 g
250 g
$31.00
$46.00
$138.00
$464.00
$903.00
(1)

Denatonium Benzoate is known as the most bitter compound and acts as a potent T2R4 agonist. By binding to T2R4, it activates the bitter taste receptor pathway, leading to an inhibition of the G-protein coupled signaling cascade that T2R4 is involved in. This results in a decreased functional activity of T2R4.

Quinine

130-95-0sc-212616
sc-212616A
sc-212616B
sc-212616C
sc-212616D
1 g
5 g
10 g
25 g
50 g
$77.00
$102.00
$163.00
$347.00
$561.00
1
(0)

Quinine is an alkaloid that can act as a bitter tastant. It can bind to T2R4 causing activation of the receptor and leading to its desensitization or internalization, thereby reducing the receptor's surface expression and functional activity.

Naringin

10236-47-2sc-203443
sc-203443A
25 g
50 g
$44.00
$99.00
7
(1)

Naringin, a flavonoid in grapefruit juice, imparts bitterness and has been shown to interact with T2R4. By stimulating the receptor, naringin can lead to receptor desensitization, reducing T2R4's responsiveness to further stimulation.

Colchicine

64-86-8sc-203005
sc-203005A
sc-203005B
sc-203005C
sc-203005D
sc-203005E
1 g
5 g
50 g
100 g
500 g
1 kg
$98.00
$315.00
$2244.00
$4396.00
$17850.00
$34068.00
3
(2)

Colchicine is a poisonous alkaloid and secondary metabolite that can modulate multiple cellular processes, including those involved in the inflammatory response. While not a direct inhibitor, it could theoretically affect T2R4 functionality by altering the cellular environment in which T2R4 operates, particularly in the context of inflammation.

Erythromycin

114-07-8sc-204742
sc-204742A
sc-204742B
sc-204742C
5 g
25 g
100 g
1 kg
$56.00
$240.00
$815.00
$1305.00
4
(3)

Erythromycin is an antibiotic that has been found to bitter and can bind to T2R4. This binding may result in receptor activation leading to a negative feedback mechanism that diminishes T2R4 activity through desensitization or reduction of receptor density on the cell surface.

Parthenolide

20554-84-1sc-3523
sc-3523A
50 mg
250 mg
$79.00
$300.00
32
(2)

Parthenolide is a sesquiterpene lactone from feverfew with known anti-inflammatory properties. It could potentially inhibit T2R4 by modulating the inflammatory pathways in which T2R4 is implicated, thereby indirectly decreasing its activation and functional response.

Caffeine

58-08-2sc-202514
sc-202514A
sc-202514B
sc-202514C
sc-202514D
50 g
100 g
250 g
1 kg
5 kg
$32.00
$66.00
$95.00
$188.00
$760.00
13
(1)

Caffeine is a bitter compound that can stimulate T2R4. Chronic exposure to caffeine could lead to T2R4 desensitization or downregulation, thereby impairing the receptor's functional activity.

D-(−)-Salicin

138-52-3sc-218004
5 g
$58.00
(0)

Salicin, a bitter-tasting compound, can activate T2R4. This activation may trigger internalization or desensitization of the receptor, reducing its activity and the subsequent signaling events.

6-Propyl-2-thiouracil

51-52-5sc-214383
sc-214383A
sc-214383B
sc-214383C
10 g
25 g
100 g
1 kg
$36.00
$55.00
$220.00
$1958.00
(0)

PTU is a thiourea derivative known for its bitter taste and potential to activate T2R4. Activation may induce a feedback mechanism leading to receptor desensitization or internalization, which decreases the functional activity of the receptor.

Sucralose

56038-13-2sc-222332
sc-222332A
100 mg
1 g
$130.00
$454.00
(0)

Sucralose is an artificial sweetener that has been reported to activate T2R4 at high concentrations. This could paradoxically lead to the inhibition of the receptor through a negative feedback loop, causing desensitization or a decrease in receptor expression on the cell surface.