Date published: 2026-4-24

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SUR-1 Inhibitors

SUR-1 inhibitors, short for Sulfonylurea receptor 1 inhibitors, belong to a specific chemical class of compounds that play a crucial role in regulating insulin secretion within pancreatic beta cells. These inhibitors target a specific protein known as the sulfonylurea receptor 1 (SUR-1), which is an integral part of the ATP-sensitive potassium (KATP) channels found in these cells. The primary function of KATP channels is to modulate the flow of potassium ions across the cell membrane, which in turn influences the electrical activity of the beta cells and insulin release. SUR-1 inhibitors exert their effects by binding to the SUR-1 subunit, thereby altering the activity of KATP channels and indirectly regulating insulin secretion.

The mechanism of action of SUR-1 inhibitors is intricately linked to their ability to block KATP channels, resulting in membrane depolarization and subsequent opening of voltage-gated calcium channels. This leads to an influx of calcium ions into the beta cells, triggering the release of insulin-containing vesicles into the bloodstream. By modulating the activity of SUR-1, these inhibitors essentially fine-tune the delicate balance between insulin production and secretion, making them valuable tools for understanding the physiological processes that underlie glucose homeostasis. Researchers and scientists have been keenly interested in studying SUR-1 inhibitors to gain insights into the intricacies of insulin regulation and its relevance in various physiological and pathological conditions, paving the way for applications in the field of diabetes research and beyond.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Diazoxide

364-98-7sc-200980
1 g
$300.00
5
(1)

Diazoxide opens the ATP-sensitive potassium channels by binding to the SUR-1 subunit, resulting in reduced insulin secretion from pancreatic beta cells. This action indirectly decreases SUR-1 expression by reducing cellular demand for this 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)

Quinine indirectly inhibits SUR-1 expression by blocking the ATP-sensitive potassium channels. This alteration in channel activity can lead to decreased stability and expression of SUR-1.

Nifedipine

21829-25-4sc-3589
sc-3589A
1 g
5 g
$59.00
$173.00
15
(1)

As a calcium channel blocker, nifedipine indirectly affects SUR-1 expression by altering intracellular calcium levels, influencing the activity and stability of the ATP-sensitive potassium channels and subsequently the SUR-1 subunit.

Glyburide (Glibenclamide)

10238-21-8sc-200982
sc-200982A
sc-200982D
sc-200982B
sc-200982C
1 g
5 g
25 g
100 g
500 g
$46.00
$61.00
$117.00
$173.00
$530.00
36
(1)

Glyburide, a sulfonylurea, binds to SUR-1, closing the ATP-sensitive potassium channels and promoting insulin secretion. Chronic exposure to glyburide may lead to a compensatory downregulation of SUR-1 expression.

Tolbutamide

64-77-7sc-203298
5 g
$44.00
2
(1)

Tolbutamide, a sulfonylurea, interacts with SUR-1 to close ATP-sensitive potassium channels. Similar to glyburide, long-term exposure to tolbutamide may result in decreased SUR-1 expression.

Chlorpropamide

94-20-2sc-234350
25 g
$73.00
7
(0)

Chlorpropamide, a first-generation sulfonylurea, interacts with SUR-1 to close ATP-sensitive potassium channels. Long-term use of chlorpropamide may lead to decreased expression of SUR-1.

Rosiglitazone

122320-73-4sc-202795
sc-202795A
sc-202795C
sc-202795D
sc-202795B
25 mg
100 mg
500 mg
1 g
5 g
$120.00
$326.00
$634.00
$947.00
$1259.00
38
(1)

Rosiglitazone, a thiazolidinedione, improves insulin sensitivity. While its primary action is on peroxisome proliferator-activated receptor gamma, it may indirectly influence SUR-1 expression through its effects on insulin signaling pathways.

Pioglitazone hydrochloride

112529-15-4sc-204848
sc-204848A
100 mg
500 mg
$63.00
$213.00
19
(2)

Pioglitazone hydrochloride, another thiazolidinedione, works similarly to rosiglitazone and may have indirect effects on SUR-1 expression through its influence on insulin sensitivity and signaling pathways.