Gefapixant(AF-219,MK-7264)
CAS 1015787-98-0
Gefapixant (AF-219, MK-7264) is a P2X3 antagonist for ATP-gated ion-channel and sensory signaling research.

Ion channels, membrane transporters and pumps.
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CAS 1015787-98-0
Gefapixant (AF-219, MK-7264) is a P2X3 antagonist for ATP-gated ion-channel and sensory signaling research.

CAS 1181081-71-9
CLP257 is a neuronal chloride-signaling research compound originally reported as a KCC2 enhancer. Subsequent work challenged direct KCC2 activation and reported GABAA receptor potentiation.

CAS 188116-07-6
AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

CAS 1163-36-6
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.

CAS 931706-15-9
PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC50 of ~90 nM.

CAS 130798-51-5
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.

CAS 2227425-05-8
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.

CAS 307510-92-5
CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibited CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.

CAS 67469-81-2
GBR 12935 2Hcl is a potent, and selective dopamine reuptake inhibitor.IC50 value: Target: dopamine reuptake inhibitorin vitro: The calculated Kd of [3H]GBR-12935 binding to CYP2D6 was 42.2 nM, indicating that GBR-12935 has a high affinity for CYP2D6. The…

CAS 148849-67-6
Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.

CAS 944261-79-4
A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7. IC50 value: 8 nMTarget: Nav1.8 sodium channelA 803467 dose-dependently reduces behavioral responses in a variety of…

CAS 448947-81-7
GlyT2-IN-1 is a glycine transporters GLYT2 inhibitor.Target: GLYT2The Glycine Transporter GlyT2 Controls the Dynamics of Synaptic Vesicle Refilling in Inhibitory Spinal Cord Neurons. GlyT2-IN-1 is a novel agonist of the mechanotransduction channel Piezo1,…

CAS 486427-17-2
CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit. IC50 value: 2.7 μM (EC50, for NR2C) and 2.8 μM (EC50, NR2D)Target: NMDA receptorCIQ increases channel opening frequency of recombinant NR2Cor NR2D containing…

CAS 25451-15-4
Felbamate (FBM) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .Felbamate (marketed under the brand name Felbatol by MedPointe) is an anti-epileptic drug used in the treatment of…

CAS 145821-59-6
Tiagabine hydrochloride(NO328 hydrochloride) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Tiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1…

CAS 328541-79-3
GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.

CAS 182004-65-5
KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM.

CAS 154235-83-3
Ampalex (Ampakine CX516; CX516; BDP 12) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

CAS 353262-04-1
NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.

CAS 675126-08-6
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

CAS 913088-80-9
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.

CAS 917393-39-6
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.Target: GABALorediplon is a drug for the treatment of insomnia, has been successfully…

CAS 1223397-11-2
WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.

CAS 2397594-21-5
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…

CAS 448895-37-2
NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 μM).

CAS 842133-18-0
Canagliflozin is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

CAS 1037592-40-7
JPH203 is a potent and selective L-type amino acid transporter 1 (LAT-1) inhibitor.

CAS 1093861-60-9
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions,…


CAS 873054-44-5
Ivacaftor is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.

CAS 167465-36-3
Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.

CAS 917837-54-8
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases…

CAS 942206-85-1
GSK1016790A is a potent transient receptor potential vanilloid 4 (TRPV4) activator.

CAS 1038984-31-4
Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.

CAS 461432-26-8
Dapagliflozin (BMS-512148) is a sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

CAS 864070-44-0
Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2..

CAS 150812-12-7
Retigabine is a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.

CAS 156223-05-1
GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation. Target: nAChRin vitro: GTS-21 is one of the most potent α7nAChR agonists, has been reported to…

CAS 115256-11-6
Dofetilide(Tikosyn) is a class III antiarrhythmic agent.In patients with congestive heart failure and reduced left ventricular function, dofetilide was effective in converting atrial fibrillation, preventing its recurrence, and reducing the risk of…

CAS 899431-18-6
A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

CAS 934240-31-0
CNV1014802(GSK-1014802) Hcl is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.IC50 value: Target: sodium channel blockerLike lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning…


CAS 5610-40-2
(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.

CAS 1019331-10-2
S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM).NBCNa(+)-coupled HCO(3)(-) transporters (NBCs) mediate the transport of bicarbonate ions across cell…

CAS 380917-97-5
Perampanel(E2007; ER 155055-90) is a selective noncompetitive AMPA-type glutamate receptor antagonist which has demonstrated anticonvulsant activity in experimental seizure models and antiepileptic activity in clinical trials.

CAS 1253452-78-6
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.IC50 value:…


CAS 141286-78-4
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
