Membrane Transporter/Ion Channel

A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.

Alfadolone acetate is a gamma-aminobutyric acid (GABA) receptor agonist.

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg/kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

PF-06761281 is a partially selective sodium-coupled citrate transporter protein (NaCT/SLC13A5) inhibitor, oral, reducing plasma glucose concentration.

2-AEMP TFA is a potent and rapidly acting antagonist of GABA(A)-ρ1 receptors. 2-AEMP is an analog of GABA.

Dexivacaine is an type of anesthetic.

2-(Trifluoromethyl)cinnamic acid is a useful organic compound for research related to life sciences. The catalog number is T64859 and the CAS number is 2062-25-1.

3-Methylglutaconic acid, a primary metabolite accumulating in 3-Methylglutaconic aciduria (MGTA), induces lipid and protein oxidation, while diminishing non-enzymatic antioxidant defenses in cerebral cortex supernatants, thereby promoting oxidative stress in the cerebral cortex. This compound is utilized in research concerning brain damage diseases [1].

Zastaprazan (JP-1366, compound 6) is a potassium-competitive acid blocker and proton pump inhibitor that suppresses gastric acid secretion, indicated for GERD.

(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a Ki of 0.56-2.1 μM for the NMDA receptor and IC50 values of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively. Lanicemine shows antidepressant effects [1].

L-Cysteine S-sulfate sodium salt sesquihydrate is a useful organic compound for research related to life sciences. The catalog number is T64782 and the CAS number is 150465-29-5.

Indoxacarb is an Oxadiazine insecticide.

NSC-609249 hydrochloride, an impurity of Verapamil, is a calcium channel blocker with potent orally active properties. It also functions as a first-generation P-glycoprotein (P-gp) inhibitor.

GNE-9278 is a highly selective NMDAR orthosteric modulator that targets the GluN1 transmembrane structural domain (TMD), enhancing peak current and agonist affinity in activated NMDAR.

Filapixant, a purinoreceptor antagonist. This compound serves as the active reference substance for Eliapixant.

CGP 44532 a GABAB receptor agonist.

TRPP3 channel inhibitor

Fostedil enhances heart function, maintains blood flow during partial/total coronary occlusions, and lowers aortic pressure.

CMPDA is a positive allosteric modulator of AMPA receptors [EC50s: 45.4 nM/63.4 nM for GluA2i/GluA2o receptor].

Gacyclidine (OTO311), an NMDA receptor blocker, treats tinnitus and injuries in the brain and spinal cord.

AKOS-22: potent VDAC1 inhibitor, Kd=15.4 μM; prevents mitochondrial dysfunction and apoptosis.

T16A(inh)-C01 is the Ca(2+)-activated Cl(-) Channel, Ano1 class C inhibitor.

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

Tifenazoxide is an effective and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.

Pipequaline (PK-8165) is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic.

Belfosdil is a blocker of antihypertensive calcium channel.

CGP 56999A is a GABA(B) receptor antagonist; it boosts BDNF and reduces dopamine loss in rat striatum.

Bumetanide sodium, a potent diuretic, blocks NKCC1 (IC50: 0.68 μM) and NKCC2 (IC50: 4.0 μM).

UBP310 (UBP 310) is a GLUK5 kainate receptor antagonist

HMR 1556 is a chromanol derivative and is an IKs blocker (IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively).