| 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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| DC70914 |
YHV98-4 |
YHV98-4 is a selective inhibitor of proton-selective ion channel Hv1 with IC50 of 0.7 uM;
YHV98-4 displays no inhibitory effects against other channels containing VSDs, including hERG, KCNQ2, BK, and Nav1.7 channel.
YHV98-4 did not inhibit transient receptor potential V1 (TRPV1) or A1 (TRPA1) at 20 uM, which also contains VSD-like domain.
YHV98-4 restores impaired ROS-mediated inflammatory pathway, restores impaired ROS-SHP-1-PI3K/pAKT-CXCL1 pathway and attenuates morphine-induced hyperalgesia and tolerance. |
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| DC70937 |
ZINC17988990
Featured
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ZINC 17988990 is a potent, selective inhibitor of TRPV5 mediated currents, inhibits rbTRPV5/hTRPV5 with IC50 of 106/177 nM, showing marked selectivity for TRPV5 over TRPV6.ZINC 17988990 shows no activity on other TRP channels (TRPV1, TRPV3, TRPV4 and TRPM8) at 1-3 uM, and moderate inhibition on TRPV3 and TRPM8 at >10 uM.ZINC17988990 (10 uM) fully inhibited Ca2+ signals elicited by application of external Ca2+ in HEK293 cells transfected with TRPV5, but had no effect in cells expressing TRPV6. |
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| DC70647 |
Neurounina-1 |
Neurounina-1 is a small molecule Na+/Ca2+ exchanger (NCX) activator, stimulates NCX1 and NCX2 activities with EC50 of 1.1-2.7 nM, does not affect NCX3 activity.Neurounina-1 (10 nM) reduced cell death of primary cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation, also reduced γ-aminobutyric acid (GABA) release, enhanced GABA(A) currents, and inhibited both glutamate release and N-methyl-d-aspartate receptors in vitro.Neurounina-1 effectively protects against stroke damage in vivo. |
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| DC70672 |
ORM-11372
Featured
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ORM‐11372 is a potent and highly selective NCX 1.1 inhibitor, inhibits human NCX 1.1 reverse and forward currents with IC50 of 5 and 6 nM respectively.ORM‐11372 weakly inhibits human cardiac sodium 1.5 (I Na) and hERG KV11.1 currents (I hERG) with IC50 of 23.2 and 10.0 uM.ORM‐11372 decreased both the outward and inward currents of hiPSC‐CMs with IC50 of 4.8 and 5.6 nM respectively, reduced the magnitude of outward I NCX (the reverse mode) in rat primary ventricular CMs with IC50 of 11.3 nM.ORM‐11372 concentration‐dependently inhibited the calcium efflux signa with an IC50 of 142 and 164 nM for experimental conditions increasing intracellular calcium and eliciting NCX forward mode activity, repectively.ORM‐11372 induced positive inotropic effects of 18 ± 6% and 35 ± 8% in anaesthetized rats with myocardial infarctions and in healthy rabbits respectively with no other haemodynamic effects. |
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| DC70754 |
SAR296968 |
SAR296968 (SAR 296968) is a potent, selective Na+/Ca2+ exchanger (NCX) inhibitor, potently inhibits hNCX1/2/3 with IC50 of 74/23/129 nM, respectively.SAR296968 showed the same range of inhibitory potency on NCX1 orthologs from dog, guinea pig, pig, rabbit, and rat (IC50=20-200 nM).SAR296968 inhibited both the forward and reverse mode of the NCX current in a concentration-dependent manner with similarly high potency in voltage-clamp studies in guinea pig cardiomyocytes.SAR296968 displays little to no effect against 5-HT2B, benzodiazepine peripheral receptor, norepinephrine uptake, dopamine uptake, AR and PR.SAR296968 exhibited antiarrhythmic properties in animal models of arrhythmias related to early or late afterdepolarizations, significantly increased left ventricular contractility in anesthetized pigs. |
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| DC70755 |
SAR340835 |
SAR340835 (SAR 340835, SAR296968 prodrug) is a potent, selective Na+/Ca2+ exchanger (NCX) inhibitor, a water-soluble prodrug of SAR296968. |
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| DC70954 |
MRS4738 |
MRS4738 is a potent and high affinity P2Y14R antagonist. MRS4738 exhibits anti-hyperallodynic and antiasthmatic activity in vivo. |
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| DC70968 |
Fenoverine |
Fenoverine is an antispasmodic drug and inhibits calcium channel currents. Fenoverine induces rhabdomyolysis. |
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| DC70970 |
IEM-1460 |
IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo. |
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| DC70982 |
(E)-4-Oxo-2-nonenal |
(E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist. |
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| DC70991 |
17-PA |
17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABAA receptors. |
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| DC70999 |
A-784168 |
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration. |
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| DC71018 |
CL 218872 |
CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABAAreceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo. |
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| DC71040 |
FEMA 4809 |
FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception. |
|
| 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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| DC71098 |
Org20599 |
Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM. |
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| DC71102 |
PGP-4008 |
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin. |
|
| DC71104 |
PPPA |
PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors. |
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| DC71110 |
S 24795 |
S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the treatment of aging-related memory disturbances. |
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| DC71153 |
Chlorisondamine diiodide |
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way. |
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| DC71169 |
AMG8788 |
AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM. |
|
| DC71170 |
AMG9678 |
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM. |
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| DC71187 |
Gavestinel sodium salt |
Gavestinel (GV 150526) is a potent, selective, orally active and non-competitive antagonist of NMDA receptor. Gavestinel binds to the glycine site of the NMDA receptor, with a pKi of 8.5. Gavestinel can be used for the research of acute ischemic stroke. |
|
| DC71241 |
HN37 |
HN37 as a potent and chemically stable antiepileptic drug candidate, with an EC50 of 37 nM for KCNQ2. |
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| DC71359 |
UR-MB108
Featured
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UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma. |
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| DC71360 |
Cav 2.2/3.2 blocker 1 |
Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC50 values of 78 μM and 80 μM against Cav2.2 and Cav3.2, respectively. Cav 2.2/3.2 blocker 1 can penetrate the CNS. |
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| DC71361 |
MONIRO-1 |
MONIRO-1 is a T-type and N-type calcium channel blocker with IC50 values of 34, 3.3, 1.7 and 7.2 µM against hCav2.2, hCav3.1, hCav3.2 and hCav3.3, respectively. |
|
| DC71362 |
DFBTA |
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain. |
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| DC71363 |
piCRAC-1 |
piCRAC-1 is a potent, photoinducible Ca2+ release-activated Ca2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage. |
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