L-type calcium channel α1C Activators
L-type calcium channel α1C Activators are a group of compounds that indirectly enhance the channel's functional activity through various mechanisms affecting calcium ion conductance. Bay K 8644, as an agonist, directly increases the influx of calcium through L-type calcium channel α1C, amplifying intracellular calcium-dependent processes. Subthreshold concentrations of Isradipine facilitate preconditioning of the channel, thus increasing its responsiveness. Similarly, FPL 64176 heightens the channel's activity by raising the open probability, while (-)-Clevidipine can, under certain conditions, induce a use-dependent facilitation of channel opening. Nifedipine's paradoxical action involves calmodulin binding to the channel, enhancing its probability of opening, and Amlodipine may sensitize the channel to activation through voltage-dependent conformational changes. Verapamil and Diltiazem, known primarily as antagonists, can exhibit use-dependent effects that favor channel activation during repetitive depolarization or channel stabilization in an activation-favorable conformation, respectively.
Further activity modulation is seen with Nicardipine, which prolongs the duration of the channel's open state,and Felodipine, which shifts the voltage dependence of activation, facilitating channel opening. Lacidipine and Manidipine both bind to the L-type calcium channel α1C, potentially inducing conformational changes that increase the likelihood of channel opening. These activators, through their specific interactions with the channel, induce a state that favors increased calcium ion permeability. This not only bolsters the channel's inherent activity but also influences the broader signaling cascades that rely on calcium signaling within the cell. The concerted action of these compounds ensures that the L-type calcium channel α1C is more readily activated, leading to an enhancement in the downstream signaling events that are critical for physiological functions such as muscle contraction, hormone secretion, and neurotransmitter release. Each compound, by fine-tuning the channel's electrical and kinetic properties, contributes to a more robust and sensitive activation profile for the L-type calcium channel α1C.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
(±)-Bay K 8644 | 71145-03-4 | sc-203324 sc-203324A sc-203324B | 1 mg 5 mg 50 mg | $84.00 $196.00 $817.00 | ||
Bay K 8644 acts as an L-type calcium channel agonist, selectively enhancing the influx of calcium ions through the L-type calcium channel α1C. This increases intracellular calcium concentrations, which in turn enhances calcium-dependent signaling pathways, thereby augmenting the functional activity of the L-type calcium channel α1C. | ||||||
Isradipine | 75695-93-1 | sc-201467 sc-201467A | 10 mg 50 mg | $88.00 $324.00 | 1 | |
Isradipine, while primarily known as a calcium channel blocker, can at subthreshold concentrations precondition the L-type calcium channel α1C, leading to an increased probability of channel opening upon subsequent depolarization events. | ||||||
Azelnidipine | 123524-52-7 | sc-252395 | 10 mg | $86.00 | ||
FPL 64176 modulates L-type calcium channels by increasing the open probability of the channel. This compound enhances calcium influx through the L-type calcium channel α1C, promoting its activity. | ||||||
Nifedipine | 21829-25-4 | sc-3589 sc-3589A | 1 g 5 g | $59.00 $173.00 | 15 | |
Nifedipine, commonly a blocker, can paradoxically enhance the activity of L-type calcium channel α1C by increasing the binding of calmodulin to the IQ domain of the channel, which is essential for the calcium-dependent facilitation of the channel's opening. | ||||||
Amlodipine | 88150-42-9 | sc-200195 sc-200195A | 100 mg 1 g | $74.00 $166.00 | 2 | |
Amlodipine binds to L-type calcium channels and can cause voltage-dependent conformational changes that may sensitize the channel to activation, thereby indirectly enhancing the functional activity of L-type calcium channel α1C. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $374.00 | ||
Verapamil, though typically a calcium channel antagonist, exhibits a use-dependent effect on L-type calcium channels, potentially enhancing the L-type calcium channel α1C activity during repetitive depolarization by affecting channel gating. | ||||||
Diltiazem | 42399-41-7 | sc-204726 sc-204726A | 1 g 5 g | $209.00 $464.00 | 4 | |
Diltiazem, also a known blocker, can indirectly enhance the activity of L-type calcium channel α1C by stabilizing the channel in a particular conformation that may favor its activation upon depolarization stimuli. | ||||||
Felodipine | 72509-76-3 | sc-201483 sc-201483A | 10 mg 50 mg | $91.00 $222.00 | 1 | |
Felodipine can enhance L-type calcium channel α1C function by shifting the voltage dependence of activation to more negative potentials, making the channel more likely to open during cellular depolarization events. | ||||||
trans Lacidipine | 103890-78-4 | sc-213066 | 10 mg | $153.00 | ||
Lacidipine binds to and modulates L-type calcium channels, potentially causing conformational changes that increase the probability of channel opening, indirectly enhancing the activity of L-type calcium channel α1C. | ||||||
Manidipine | 89226-50-6 | sc-211774 | 10 mg | $278.00 | ||
Manidipine interacts with L-type calcium channels and may facilitate their opening by altering channel kinetics, which would indirectly increase the functional activity of L-type calcium channel α1C. | ||||||