| DC70542 |
KNa1.1 inhibitor 31 |
KNa1.1 inhibitor 31 is a potent, selective, orally available inhibitor of sodium-activated potassium channel KNa1.1 (Slack, Slo2.2) with IC50 of 40 nM (hKNa1.1 WT).KNa1.1 inhibitor 31 reduced seizures and interictal spikes in a mouse model of KCNT1 GoF. |
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| DC70552 |
Kv2.1-syntaxin inhibitor 15 |
Kv2.1-syntaxin inhibitor 15 (Kv2.1-syntaxin-IN-15, Cpd5) is a small molecule Kv2.1-syntaxin-binding inhibitor (IC50=5.5 uM) with neuroprotective properties.Kv2.1-syntaxin inhibitor 15 competitively binds syntaxin against C1aB-containing Kv2.1 peptides with IC50 of 5.5 uM.Kv2.1-syntaxin inhibitor 15 (10 uM) significantly diminished threo-β-benzyloxyaspartate (TBOA, 75 uM)-induced toxicity neuronal cultures, ameliorated significant cellular damage, by preventing the expression of enhanced Kv2.1-mediated K+ currents.Kv2.1-syntaxin inhibitor 15 is a first-in-class inhibitor of Kv2.1 binding to Syntaxin, likely due to inhibition of the C1a region of Kv2.1 binding to syntaxin.Cpd5 (10 μM) does not affect evoked AMPAR EPSCs in layer 2/3 corticocallosal neurons in the mouse auditory cortex. |
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| DC70574 |
Lu AA41178
Featured
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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. |
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| DC70890 |
VU0606170 |
VU 0606170 is a selective sodium-activated potassium channel KNa1.1 (Slack, Slo2.2) inhibitor with EC50 of 1.84 and 1.16 uM for WT Slack and A934T Slack, repectively.VU0606170 did not modulate HEK293 channels expressing Slick, Slo1 α1/β1, Slo1 α1/β2, Slo1 α1/β3, Slo1 α1/β4, or Slo3 channels. also potently inhibits G288S and R428Q Slack channels.VU0606170 also proved effective at significantly decreasing the firing rate in overexcited, spontaneously firing cortical neuron cultures. |
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| DC70892 |
VU0468554 |
VU0468554 (VU 0468554) is a nove potent, selective inhibitor of GIRK channel with IC50 of 0.85 and 2.6 uM for GIRK1/GIRK4 and GIRK1/GIRK2 in cellular assays.VU0468554 more effectively inhibits the cardiac GIRK channel than the neuronal GIRK channel, inhibits Gβγ-activated GIRK channels in noncompetitive and potentially uncompetitive fashion.VU0468554 competitively inhibits GIRK-channel activation by ML297, a GIRK-channel activator.In the isolated heart model, VU0468554 partially reversed carbachol-induced bradycardia in hearts from wild-type mice but not Girk4-/- mice. |
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| DC70898 |
VU6036720 |
VU6036720 (VU 6036720) is the first potent, selective inhibitor of heteromeric Kir4.1/Kir5.1 (KCNJ10/KCNJ16) with IC50 of 0.24 uM.VU6036720 displays >30-fold selective for Kir4.1/5.1 over homomeric Kir4.1 channels, Kir1.1, Kir2.1, Kir2.2, Kir2.3, Kir4.2, Kir6.2/SUR1, Kir6.1/SUR2b and Kir7.1.VU6036720 inhibits Kir4.1/5.1 activity through a reduction of channel open-state probability and single-channel current amplitude, does not induce diuresis in vivo.VU6036720 showwd an IC50 in 3 uM in Tl+ flux assays, approximately 7-times more potent at inhibiting Kir4.1/5.1 than fluoxetine and amitriptyline.VU6036720 represents the current state-of-the-art Kir4.1/5.1 inhibitor that should be useful for probing the functions of Kir4.1/5.1 in vitro and ex vivo. |
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| DC70907 |
XAF-1407 |
XAF-1407 (XAF1407) is a novel putatively potent and highly specific IK,Ach (Kir3.1/3.4 and Kir3.4/3.4) inhibitor (IC50 of 1.1 and 3.2 nM, respectively).XAF-1407 displays highly selectivity other relevant cardiac ion channels, with selectivity ratios for Kir3.1/3.4 of >2,000–8,000 fold up to >27,000 fold for Nav1.5 and Kir2.1, respectively.XAF-1407 potently and selectively inhibited Kir 3.1/3.4 and Kir 3.4/3.4, underlying the IK,ACh current.XAF-1407 treatment in horses prolonged atrial effective refractory period as well as decreased atrial fibrillatory rate significantly and successfully cardioverted atrial fibrillation (AF), although with a decreasing efficacy over time. XAF-1407 shortened atrioventricular-nodal refractoriness, without effect on QRS duration. |
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| DC71047 |
GAL-021 sulfate |
GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates. |
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| DC71241 |
HN37 |
HN37 as a potent and chemically stable antiepileptic drug candidate, with an EC50 of 37 nM for KCNQ2. |
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| DC71368 |
DDO-02005 |
DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine. |
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| DC71369 |
DDO-02001 |
DDO-02001 is a moderately potent Kv1.5 potassium channel inhibitor with an IC50 value of 17.7 μM. DDO-02001 can be used for researching anti-arrhythmia. |
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| DC71370 |
DDO-02005 free base |
DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine. |
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| DC71371 |
Dendrotoxin K |
Dendrotoxin K is a Kv1.1 channel blocker. Dendrotoxin K determines glutamate release in CA3 neurons in a time-dependent manner through the control of the presynaptic spike waveform. |
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| DC71372 |
PBFI-AM |
PBFI-AM is a useful tool to determine intracellular K+ content. |
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| DC71373 |
Mitiglinide |
Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes. |
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| DC71374 |
N-Bromoacetamide |
N-Bromoacetamide can irreversibly remove sodium channel inactivation in the cytoplasmic face of the membrane, also decreasing K current rapid inactivation. |
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| DC72050 |
NS-8 |
NS-8, a pyrrole derivative, activates the Ca2+-sensitive k+-channel. NS-8 can suppress the micturition reflex by decreasing afferent pelvic nerve activity. NS-8 can be used in the research of urinary frequency and incontinence. |
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| DC72215 |
Clobutinol |
Clobutinol is a compound that has anti-tussive effects. Clobutinol affects heart rate and blood pressure, it can be used for cough related research. |
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| DC72362 |
TRAM-39 |
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease. |
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| DC72363 |
β-Bag cell peptide |
β-Bag cell peptide is a neuroactive peptide. β-Bag cell peptide elevates cyclic AMP levels in the bag cell neurons. β-Bag cell peptide decreases the amplitudes of the voltage-dependent potassium currents. |
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| DC72655 |
Foslevcromakalim |
Foslevcromakalim (QLS-101) is a ATP-sensitive potassium channel opener. Foslevcromakalim is the prodrug used for ocular hypotensive effect. |
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| DC72656 |
Etidocaine Hydrochloride |
Etidocaine (hydrochloride) is a long aminoamide local anaesthetic that inhibits flicker potassium channel with an IC50 of 8.6 µM. |
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| DC72866 |
ML-213 |
ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively.
ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5).
ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels. |
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| DC73659 |
3hi2one-G4 |
3hi2one-G4 is a highly selective small molecule activator targeting GIRK4 homomeric channels, does not activate GIRK2, GIRK1/2 or GIRK1/4 channels. |
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| DC73660 |
ACOU001 |
ACOU001 (ACOU 001) is a potent small-molecule agonist of Kv7.4 (KCNQ4) channel with potential effect against ge-related hearing loss (ARHL) and other hearing impairments related to compromised KV7.4 function. |
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| DC73661 |
ACOU085 |
ACOU085 (ACOU 085) is a potent small-molecule agonist of Kv7.4 (KCNQ4) channel with higher potency than ML-213 in the nanomolar range. |
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| DC73662 |
AUT00201 |
AUT00201 is a potent, selective Kv3 potassium channel modulator with potential for the treatment of rare epilepsy syndromes. |
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| DC73663 |
BK channel modulator BC5 |
BK channel modulator BC5 is an allosteric modulator of BK type Ca2+-activated K+ channels, interacts with the CTD-VSD interface and specifically modulates the Ca2+ dependent activation mechanism. |
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| DC73664 |
C101248 |
C101248 is the first selective small-molecule inhibitor of tandem pore domain halothane-inhibited K+ channel 1 (THIK-1) with IC50 of 50 nM for both mouse and human THIK-1. |
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| DC73665 |
KCNQ2 activator Ebio1
Featured
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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). |
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