| DC73675 |
VU0546110
|
VU0546110 (VU 0546110) is a potent, selective inhibitor of the sperm-specific potassium channel SLO3 with IC50 of 1.29 uM, impairs sperm function. |
| DC73665 |
KCNQ2 activator Ebio1
|
Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV). |
| DC70574 |
Lu AA41178
|
Lu AA41178 is a potent, pan-selective Kv7.2-7.5 opener with EC50 of 1.5, 0.6 20.5, and 37.0 uM for Kv7.2, Kv7.2/7.3, Kv7.4 and Kv7.5, respectively.Lu AA41178 displays no activity at Kv7.1 channels, has no potentiating impact on currents through GABAA ion channels, and a clean off-target profile against common cardiac ion channels.Lu AA41178 significantly increased the seizure thresholds in mice, demonstrating anticonvulsant efficacy in the maximum electroshock seizure threshold test and PTZ seizure threshold test.Lu AA41178 demonstrated antipsychotic-like activity by reducing amphetamine-induced hyperlocomotion in mice as well as lowering conditioned avoidance responses in rats, significantly reduced immobility in mouse model with antidepressant predictivity. |
| DC70426 |
GAT1508
|
GAT1508 (GAT-1508) is a potent, specific activator for brain-expressed GIRK1/2 channels (EC50=75 nM), specifically activates the brain GIRK1/2 over the cardiac GIRK1/4;
GAT1508 is an allosteric modulator of channel–phosphatidylinositol 4,5-bisphosphate interactions.
GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder. |
| DC48873 |
DPO-1
|
DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of ultrarapid delayed rectifier potassium current. DPO-1 prevents atrial arrhythmia. |
| DC47376 |
Rimtuzalcap
|
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA). |
| DC41224 |
Minoxidil sulfate
|
Minoxidil sulfate, a potent and ATP-sensitive K+ channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo. |
| DC41048 |
A2793
|
A2793 is an efficient TWIK-related acid-sensitive K+ channel (TASK)-1 inhibitor, with an IC50 of 6.8 μM. |
| DC39089 |
H3B-120
|
H3B-120 is a competitive, selective and allosteric inhibitor of carbamoyl phosphate synthetase 1 (CPS1) with IC50 of 1.5 μM and Ki of 1.4 μM. H3B-120 exhibits anti-tumor activity. |
| DC28951 |
A2764 dihydrochloride
|
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception. |
