HUP30 is a vasodilating agent. HUP30 stimulates soluble guanylyl cyclase, activate K+ channels, and blocks extracellular Ca2+ influx[1].
MV1035 (MV-1035) is a novel small molecule that reduce U87 GBM cells migration and invasiveness, targeting m6A demethylase ALKBH5, also inhibits ALKBH2;MV1035 directly inhibits active recombinant ALKBH5 protein and, consequently, negatively regulates CD73 protein expression without affecting CD73 mRNA transcription.In PD-GSCs, MV1035 has a synergistic effect with TMZ in reducing cell viability and their ability to form spheres.MV1035 is able both to reduce the expression of MGMT and to inhibit ALKBH2 activity.
Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
Dizocilpine, a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux[1][2].
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM.
Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease[1][2].
Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease[1][2][3].
AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1].
Esomeprazole magnesium is an inhibitor of H+, K+-ATPase, effectively used in the research of upper intestinal disorder.
CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity[1].
Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM[1].
Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain[1].
LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract[1].
Mitiglinide calcium hydrate is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. IC50 value:Target: KATP channel
(rel)-ML-SI3 is the isomer of ML-SI3 (HY-139426). ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy[1][2].
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons[1][2].
Xilmenolone is a GABAA receptor positive allosteric modulator[1].
PTI-428 is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier[1].
Foslevcromakalim (QLS-101) is a ATP-sensitive potassium channel opener. Foslevcromakalim is the prodrug used for ocular hypotensive effect[1][2].
LY-466195 is a competitive antagonist of GLUK5 receptor.
Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.Target: GABA ReceptorBaclofen, a lipophilic analog of gamma-aminobutyric acid, is clinically used to control spasticity. Baclofen pretreatment (3 mg/kg) not only prolonged the time taken for animals to reach a core body temperature of 40 degrees C (P < 0.001), but also reduced the percentage of rats attaining a core body temperature of 40 degrees C [1]. Baclofen overdose may result in coma, apnea, autonomic disturbances, cardiac conduction abnormalities, and seizures. Levels obtained shortly after overdose correlate with length of mechanical ventilation [2].
Norbormide shows vasoconstrictor activity by blocking calcium channel. The activity of Norbormide is species- and tissue-specific, endothelium independent, and is restricted to the peripheral arteries of rat. Norbormide is also a toxicant, and the oral LD50s in mouse, hamster, guinea pig and rabbit are 2250, 140, 620, and 1000 mg/kg[1].
Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM[1][2].
SOICR-IN-1 (compound 32) is a store-overload induced calcium release (SOICR) inhibitor with an IC50 value of 14.6 μM. SOICR-IN-1 can be used for the research of cardiac arrhythmias[1].
GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1[1][2].
Cinnarizine is an antihistamine and a calcium channel blocker, promote cerebral blood flow, used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis.
BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation[1].
ISX-9 is a small molecule inducer of adult neural stem cell differentiation. Target: At 2.5-20 μM, ISX-9 has been shown to dose-dependently trigger neurogenesis and block gliogenesis in adult rat hippocampal stem cells through a calcium-activated signaling pathway dependent on myocyte-enhancer factor 2-dependent gene expression.ISX-9 administered at 20 mg/kg for 12 days to mice has been reported to improve hippocampal function as evidenced by enhanced spatial memory ability in the Morris water maze test.