NMDAR/TRPM4 inhibitor 19 (Compound 19)
CAS 1456994-27-6
NMDAR/TRPM4 inhibitor 9 (Compound 9) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.
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HC-067047
CAS 883031-03-6
HC-067047 is a potent and selective TRPV4 antagonist with IC50s of 48 nM, 133 nM, and 17 nM for human, rat, and mouse TRPV4.
TCS 5861528
CAS 332117-28-9
TCS 5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively).
KGA-2727
CAS 666842-36-0
KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2; attenuates the elevation of plasma glucose after glucose loading in streptozotocin-induced diabetic rats, preserves glucose-stimulated insulin secretion and…
Varenicline tartrate
CAS 375815-87-5
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.Varenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking addiction. As a…
Deudextromethorphan
CAS 1079043-55-2
Deudextromethorphan (AVP-786) is a deuterated form of dextromethorphan/quinidine (AVP-923, Nuedexta). Deudextromethorphan, a glutamate-targeting agent, is an orally active N-methyl-D-aspartate (NMDA) receptor antagonist. Deudextromethorphan can be used for…
Tezacaftor(VX661)
CAS 1152311-62-0
VX-661 is a second F508del CFTR corrector and help CFTR protein reach the cell surface.
Lesinurad (RDEA594）
CAS 878672-00-5
Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
Sotagliflozin (LX-4211)
CAS 1018899-04-1
LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.IC50 value:Target: SGLT1/2LX4211 enhanced urinary glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic…
RU-TRAAK-2
CAS 1210538-56-9
RU-TRAAK-2 is a completely reversible TRAAK inhibitor, shows no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).
PAP-1
CAS 870653-45-5
PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]
BI-749327
CAS 2361241-23-6
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus T
Imidazole ketone erastin（IKE）
CAS 1801530-11-9
Imidazole ketone erastin (IKE) s a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system Xc- and an activator of ferroptosis.
UoS12258
CAS 875927-64-3
UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6; displays excellent wide selectivity against a wide range of other ion channels (including hERG, NMDA, and kainate channels), enzymes, and GPCRs;…
ML-SI3
CAS 891016-02-7
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.
Elexacaftor
CAS 2216712-66-0
Elexacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). CFTR corrector 1 (compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface[1].
Chlorotoxin
CAS 163515-35-3
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
ARN23746(IAMA-6)
CAS 2497525-96-7
ARN 23746 (ARN-23746) is a potent, selective inhibitor of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and…
Jamaicin (AnCoA4)
CAS 24211-36-7
AnCoA4 (AnCoA-4, AnCoA 4) is a potent Orai1 channel inhibitor that inhibits store-operated calcium (SOC) with EC50 of 0.88 uM; binds to the C terminus of Orai1, directly inhibits calcium influx through the channel and also reduces binding of STIM1; decreased…
LY 3130481
CAS 1610802-47-5
LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members; demonstrates fully protective against pentylenetetrazole-induced…
TRPC6-PAM-C20
CAS 667427-75-0
TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6…
AM-0902
CAS 1883711-97-4
AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.
Dalzanemdor
CAS 1629853-48-0
Dalzanemdor (SAGE-718) is a N-methyl-D-aspartate (NMDA) receptor positive allosteric modulator.
Lacosamide
CAS 175481-36-4
Lacosamide is a functionalized amino acid that produces activity in the maximal electroshock seizure (MES) test, that, like some other antiepileptic drugs (AEDs), are believed to act through voltage-gated sodium channels. Lacosamide enhances the slow…
S9-A13
CAS 1223771-84-3
S9-A13 is a highly potent and specific inhibitor of SLC26A9, potently inhibits SLC26A9-mediated Cl−/I− and Cl−/SCN− exchange activities with IC50 of 90.9 and 171.5 nM, respectively.S9-A13 does not inhibit other members of the SLC26 family and has no effects…
Solriamfetol hydrochloride
CAS 178429-65-7
Solriamfetol (JZP-110) is a selective dopamine and norepinephrine reuptake inhibitor with robust wake-promoting effects. Solriamfetol binds to dopamine and norepinephrine transporters, so it can inhibit reuptake of dopamine and norepinephrine. Solriamfetol…
CLP-290
CAS 1181083-81-7
CLP290 is an orally available activator of the neuron-specific K+-Cl− cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose…
Bay K-8644
CAS 71145-03-4
Bay K 8644, a dihydropyridine compound, is a specific L-type Ca2+ channel agonist. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca2+ channels by increasing the open time of the channel[1].
Pregabalin
CAS 148553-50-8
For the detailed information of Pregabalin, the solubility of Pregabalin in water, the solubility of Pregabalin in DMSO, the solubility of Pregabalin in PBS buffer, the animal experiment（test） (test) of Pregabalin, the cell expriment (test) of Pregabalin, the…
Esomeprazole sodium
CAS 161796-78-7
Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.Esomeprazole sodium (Nexium) is the S-isomer of omeprazole and acts as a proton pump inhibitor and gastric…
Isradipine
CAS 75695-93-1
Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and…
TRPM4 inhibitor 5
CAS 351424-20-9
TRPM4 inhibitor 5 is a potent and selective inhibitor of TRPM4 with IC50 of 1.5 uM (Na+ influx); selectively inhibits TRPM4 overexpressed in HEK293 cells (IC50=1.8 uM) using classical patch-clamp electrophysiology recordings, shows no significant effect on…
TRPM4-IN-2
CAS 667411-04-3
TRPM4-IN-2 (NBA) is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC50 value of 0.16 μM. TRPM4-IN-2 can be used for researching prostate cancer and colorectal cancer[1][2].
LTGO-33
CAS 2834106-06-6
LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.
Dasotraline(SEP-225289) free base
CAS 675126-05-3
Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
NVS-ZP7-4
CAS 2349367-89-9
NVS-ZP7-4 is a potent ZIP7 Inhibitor, which inhibits Notch signaling with IC50 of 0.13 uM in HES-Luc reporter gene assays, selectively induces apoptosis and ER stress. NVS-ZP7-4 altered zinc in the ER, and an analog of the compound photoaffinity labeled ZIP7…
ORM-11372
CAS 2376217-14-8
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…
Retigabine dihydrochloride
CAS 150812-13-8
Retigabine (D-23129) is a novel antiepileptic compound with broad spectrum and potent anticonvulsant properties, both in vitro and in vivo. The compound was shown to activate a K+ current in neuronal cells. The pharmacology of the induced current displays…
Indiplon
CAS 325715-02-4
Potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7 nM in rat frontal cortex and cerebellum respectively). Displays ~ 10-fold selectivity for α1 subunit-containing receptors (EC50 values are 2.6,…
Ilaprazole
CAS 172152-36-2
Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
Ranolazine (Ranexa)
CAS 95635-55-5
Ranolazine is an antianginal medication.Target: Sodium ChannelRanolazine is believed to have its effects via altering the transcellular late sodium current. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the…
LDN-212320
CAS 894002-50-7
LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.IC50 value: 1.83 uM(EC50) [2]Target: EAAT2 activatorin vitro: LDN/OSU-0212320 increased EAAT2 protein levels in a…
PF-01247324
CAS 875051-72-2
PF-01247324 is an orally bioavailable, selective and potent NaV1.8 channel blocker that inhibits that exhibits analgesic efficacy in rodent behavioral models of pain.
Senicapoc
CAS 289656-45-7
Senicapoc (ICA-17043) is a potent and selective Gardos channel blocker with IC50 value of 11 nM. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
ICA-121431
CAS 313254-51-2
ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.IC50 value: 19 nM (rat Nav1.7) [1]Target: rat Nav1.7 inhibitorICA-121431 exhibited a spectrum of…
NS309
CAS 18711-16-5
NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.IC50 value: Ca2+-activated K+ channelTarget:
PF-04971729 (Ertugliflozin)
CAS 1210344-57-2
Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[1]. A drug for the treatment of type 2 diabetes mellitus[2].
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