Date published: 2025-12-19

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RyR-1 Inhibitors

RyR-1 (ryanodine receptor 1) inhibitors represent a class of chemical compounds characterized by their ability to modulate the activity of the ryanodine receptor subtype 1, a calcium ion channel predominantly found in skeletal muscle cells. These inhibitors are primarily used as research tools to investigate the intricate mechanisms governing calcium ion release and homeostasis within muscle cells. Understanding the functioning of RyR-1 is essential because aberrant calcium regulation can lead to muscle-related disorders, including malignant hyperthermia and various myopathies. At the molecular level, RyR-1 inhibitors exhibit a diverse range of chemical structures and mechanisms of action. They often interact with specific binding sites on the RyR-1 protein, altering its conformation or blocking its function. Some inhibitors stabilize the closed state of the RyR-1 channel, preventing the release of calcium ions from the sarcoplasmic reticulum, which is vital for muscle contraction. Others act as antagonists or modulators, influencing the channel's response to intracellular signals. While these inhibitors serve as valuable tools for dissecting the role of RyR-1 in muscle physiology, their use requires careful consideration due to the delicate balance of calcium regulation in muscle cells and off-target effects. In research settings, RyR-1 inhibitors are indispensable for elucidating the complexities of calcium signaling in muscle contraction and relaxation. By selectively targeting RyR-1, scientists can explore the receptor's role in normal muscle function and pathological conditions. Nonetheless, their precise mechanisms of action and safety profiles necessitate rigorous investigation and thoughtful application in scientific studies to ensure accurate and meaningful findings without inadvertently interfering with essential cellular processes.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Dantrolene sodium salt

14663-23-1sc-202124
100 mg
$73.00
9
(1)

Dantrolene sodium salt (CAS 14663-23-1) is a RyR-1 inhibitor that hinders calcium ion release from the sarcoplasmic reticulum in muscle cells.

Dantrolene, Sodium Salt Hemiheptahydrate

24868-20-0sc-218075
100 mg
$115.00
(0)

Dantrolene, Sodium Salt Hemiheptahydrate (CAS 24868-20-0) acts as an inhibitor of RyR-1, influencing calcium ion release in muscle cells.

Ruthenium red

11103-72-3sc-202328
sc-202328A
500 mg
1 g
$184.00
$245.00
13
(1)

This chemical compound is a non-specific inhibitor of ryanodine receptors, including RYR-1. It can block the release of calcium ions from the sarcoplasmic reticulum, affecting muscle contraction.

FK-506

104987-11-3sc-24649
sc-24649A
5 mg
10 mg
$76.00
$148.00
9
(1)

FK-506 indirectly affects RYR-1 by inhibiting calcineurin, a protein phosphatase that regulates calcium release from the sarcoplasmic reticulum.

Nifedipine

21829-25-4sc-3589
sc-3589A
1 g
5 g
$58.00
$170.00
15
(1)

Nifedipine is a calcium channel blocker. It indirectly inhibits RYR-1 by reducing the influx of calcium ions into muscle cells.

Fluoxetine

54910-89-3sc-279166
500 mg
$312.00
9
(1)

This has been studied for its potential to inhibit RYR-1 and reduce abnormal calcium release in muscle cells.

Sorafenib

284461-73-0sc-220125
sc-220125A
sc-220125B
5 mg
50 mg
500 mg
$56.00
$260.00
$416.00
129
(3)

Sorafenib is a multi-kinase inhibitor. It has been investigated for its effect on RYR-1 channels.

Ryanodine

15662-33-6sc-201523
sc-201523A
1 mg
5 mg
$219.00
$765.00
19
(2)

Ryanodine is an alkaloid found in plants. It is a high-affinity ligand for the ryanodine receptor, but it acts as an agonist rather than an inhibitor. When used, it activates RYR-1, leading to calcium release and muscle contraction.

CGP 37157

75450-34-9sc-202097
sc-202097A
5 mg
25 mg
$113.00
$454.00
3
(1)

CGP-37157 is a mitochondrial Na+/Ca2+ exchanger inhibitor. It indirectly affects RYR-1 by influencing calcium homeostasis in muscle cells.