Membrane Transporter/Ion Channel

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

(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.

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

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.

Indoxacarb is an Oxadiazine insecticide.

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].

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]

<p>Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase.</p>

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

<p>Motugivatrep is a potent and selective TRPV1 antagonist that can be used to study TRPV1-related respiratory diseases.</p>

TRPP3 channel inhibitor

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

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

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

CGP 44532 a GABAB receptor agonist.

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.

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

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

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.