A 804598
CAS 1125758-85-1
A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.
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Varenicline
CAS 249296-44-4
Varenicline(CP 526555;Champix) is a selective α4β2 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…
Saclofen
CAS 125464-42-8
Saclofen is a competitive antagonist of the GABAB receptor with an IC50 of 7.8 μM. Saclofen can be used to determine the functional roles for the GABAB receptor as a mediator of slow inhibitory postsynaptic potentials in the brain[1].
NS638
CAS 150493-34-8
NS-638 is a small nonpeptide molecule with Ca2+-channel blocking properties. K+-stimulated intracellular Ca2+-elevation is blocked with an IC50 value of 3.4 μM.
7ACC2
CAS 1472624-85-3
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.IC50 value: 11 nM ([14C]-lactate influx) [1]Target: MCT inhibitor; lactate transport…
DAA1106
CAS 220551-92-8
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.Target:PBRin vitro: DAA1106 binding to PBR was significantly increased in widespread areas in…
KM 11060
CAS 774549-97-2
KM11060 is a novel corrector of the F508del-CFTR trafficking defect.Target: CFTRin vitro: Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing defect and in the development of cystic…
Fluralaner
CAS 864731-61-3
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
NS11394
CAS 951650-22-9
NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
Pipequaline
CAS 77472-98-1
Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.
(-)MK-801 maleate
CAS 121917-57-5
(-)-MK 801 Maleate is the enantiomer of (+)-MK-801. (+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist.
(+)MK-801 maleate
CAS 77086-22-7
(+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
DNQX
CAS 2379-57-9
DNQX is a AMPA receptor antagonists.target: AMPA receptorIn vitro: DNQX, added 2 h after cell plating, induces a dose-dependent neurotoxicity.
CNQX disodium salt
CAS 479347-85-8
CNQX is a potent AMPA/kainate receptor antagonist. Also antagonist at glycine modulatory site on NMDA receptor complex.
DNQX disodium salt
CAS 1312992-24-7
DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively)[1].
SB-705498
CAS 501951-42-4
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
SB-366791
CAS 472981-92-3
SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nM. SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis…
DS-1971a
CAS 1450595-86-4
DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects[1].
ML-SA5
CAS 2418670-70-7
Novel mucolipin 1 (ML1) agonist, inducing lysosomal Ca2+ release, ameliorating muscular dystrophies and activating TFEB to correct lysosomal insufficiency in mdx mice
A-317491 (sodium salt hydrate)
CAS 475205-49-3
A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3…
rac BHFF
CAS 123557-91-5
rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor[1].
GDC-0334
CAS 1984824-54-5
GDC-0334 (GDC0334) is a highly potent, selective, orally bioavailable TRPA1 antagonist with IC50 of 1.7 nM in cell-based assays.GDC-0334 demonstrated potent TRPA1 inhibition in several species, including human (IC50=1.7 nM), cynomolgus (IC50=3.6 nM), mouse…
Bumetanide
CAS 28395-03-1
Bumetanide(Ro 10-6338; PF 1593) is an inhibitor of Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 uM.
AMG517
CAS 659730-32-2
AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.
TRCP6 inhibitor(SAR7334)
CAS 1333207-63-8
SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
ABT-639
CAS 1235560-28-7
ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
NS 9283
CAS 913830-15-6
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's…
UCPH-101
CAS 1118460-77-7
UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
AF-353(Ro-4)
CAS 865305-30-2
AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).
QNZ(EVP4593)
CAS 545380-34-5
QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.
Zuranolone
CAS 1632051-40-1
Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor.
BAY-876
CAS 1799753-84-6
BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.
CALCIUM IONOPHORE II
CAS 74267-27-9
N,N,N′,N′-Tetracyclohexyl-3-oxapentanediamide (Calcium ionophore II) is a lipophilic ionophore that can be used in preparing calcium ion-selective electrode[1].
JNJ-17203212
CAS 821768-06-3
JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.
PF 05089771
CAS 1235403-62-9
PF 05089771 is a Nav1.7 channel blocker extracted from patent WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 nM.
HM30181 mesylate
CAS 849675-87-2
HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.
Talampanel (GYKI 53773)
CAS 161832-65-1
Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED).
ML-277
CAS 1401242-74-7
ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.ML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the…
AMG9810
CAS 545395-94-6
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
SLC25A1 inhibitor CTPI-2
CAS 68003-38-3
CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis,…
Cabotegravir(GSK744)
CAS 1051375-10-0
Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).IC50 value: 0.81 μM (OAT1),…
AZ-1
CAS 803735-54-8
AZ-1 is a small molecule inducer of ABCA1 and apoE that act through indirect activation of the LXR pathway, shows purinergic receptor P2X7 antagonist activity; upregulates ABCA1 across multiple CNS cell types, including human astrocytes, pericytes, and…
CNV1014802(Raxatrigine)
CAS 934240-30-9
CNV1014802(GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.sodium channel blockerLike lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus…
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