Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
Calcicludine is a protein toxin from the venom of the green mamba Dendroaspis angusticeps that inhibits high-voltage-activated calcium channel, especially L-type calcium channel with the IC50 of 88 nM. Calcicludine has role in excitatory synaptic transmission[1][2].
(-)-Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker. It is an alkaloid, can chelate the bivalents calcium and magnesium.
Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Galicaftor can be used for cystic fibrosis research[1].
(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site[1].
Remimazolam (CNS-7056) is a short-acting GABA(A) receptor agonist[1].
Inaperisone is a centrally acting muscle relaxant. Inaperisone inhibits the micturition reflex by acting indirectly on GABAB receptors in the brainstem[1].
PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors[1][2].
trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a very potent and selective NMDA receptor agonist that modulates glutamatergic neurotransmission[1].
Glycerophosphoinositol choline is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders[1][2].
MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research[1].
Chromanol 293B is a selective blocker of the slow delayed rectifier K+ current (IKs) with IC50 of 1-10 μM and a weak inhibitor of KATP channel. Chromanol 293B also blocks the CFTR chloride current with an IC50 of 19 μM[1].
Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations[1].
LY 392098 is a selective, potent and centrally active positive allosteric modulator of AMPAR; enhances glutamate (100 uM) stimulated ion influx through recombinant homomeric human AMPAR ion channels with EC50 of 1.77 uM (GluR1(i)), 0.22 uM (GluR2(i)), 0.56 uM (GluR2(o)), 1.89 uM (GluR3(i)) and 0.20 uM (GluR4(i); enhances a dose-dependent manner responses to AMPA, potentiates the synaptic excitation of dentate granule cells following perforant path stimulation in vivo.
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization[1][2].
PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade[1].
Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure[1].
μ-Conotoxin BuIIIC (Mu-Conotoxin BuIIIC) is a potent Nav1.4 inhibitor[1].
Decanoic acid-d19 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
Esomeprazole potassium salt is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.IC50 value:Target: proton pumpEsomeprazole potassium salt is a proton pump inhibitor and gastric antisecretory agent indicated for the short-term treatment of gastroesophageal reflux disease in patients with a history of erosive esophagitis.
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][5][6].
L-Ascorbic acid-13C-2-4 is the 13C labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collag
Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice[1].
DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC), voltage-dependently activates potassium channels TREK1 and TRAAK, inhibits TRESK, TASK1 and TASK3 (IC50s, 0.14, 0.95, 50.72 μM, respectively)[1]. DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM in CPAE cells[2].
7-Chlorokynurenic acid sodium salt is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex and also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM.
Doxacurium chloride (BW A938U) is a potent non-depolarizing neuromuscular blocking agent. Doxacurium chloride binds to cholinergic receptors to antagonize acetylcholine, resulting in a block of neuromuscular transmission. Doxacurium chloride can be used for the research of neurological diseases[1].
TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes[1][2].
Bumetanide(Ro 10-6338; PF 1593) is an inhibitor of Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 uM.IC50 Value: 0.6 uM [1]Target: NKCC (Na-K-Cl cotransporter)in vitro: Cultured chick cardiac cells possess a Na+K+Cl-co-transport system that is inhibited by the "loop diuretics" bumetanide (IC50 = 0.6 microM). The K0.5 values for Cl- and Na+ activation of thebumetanide-sensitive 86Rb+ uptake are 59 mM and 40mM respectively. Bumetanide also inhibits a 22Na+ uptake component that is suppressed when external Cl- or K+ are substituted by impermeant ions. The ratio of bumetanide-sensitive 86Rb+ to 22Na+ uptake is close to 1. The cardiac Na+/K+/Cl- cotransport is a major uptake pathway for Na+ and K+ [1]. Bumetanide inhibits ouabain-resistant 86Rb(K+) influx with IC50of 0.1, 5.0, and 0.05 microM for J774.2, CT2 and J7H1 macrophages, respectively [2]. in vivo:Intraperitoneal injection of 50 or 100 mg bumetanide/kg body weight resulted in an acute and transient hyperglycaemia. Pretreatment with 240 mg probenecid/kg body weight reduced the diuretic effect but potentiated the hyperglycaemic effect of bumetanide (50 mg/kg body weight). The glucose tolerance was impaired, and there was an elevated serum glucose and glucose/insulin ratio 2 h after a single injection of bumetanide (100 mg/kg body weight) [3].