potentiator

VU-29 is a positive allosteric mGlu5 receptor modulator with an EC50 of 9 nM and a Ki of 244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes [EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM].

CFTRpotentiator 1 (I1421) is a potent CFTR potentiator with an EC50 value of 64 nM. It allosterically activates various mutations causing cystic fibrosis, such as ΔF508 and G551DCFTR.

Bradykinin potentiator-5 is a peptide inflammatory mediator, causes blood vessels to dilate (enlarge), and therefore causes blood pressure to fall.

OV-potentiator-28 is a potentiator of cancer virotherapy. OV-potentiator-28 significantly enhances virus replication-associated luciferase expression, specifically in tumors.

NMDA receptor potentiator-1 (Compound 1368) is a subunit-selective NMDA receptor enhancer with IC50 values of 4 μM for NR2C and 5 μM for NR2D expression.

Bradykinin Potentiator B (also known as Bradykinin Potentiating Peptide B), derived from the venom of Agkistrodon halys blomhoffi, serves as a potent ACE inhibitor. It effectively inhibits the activity of bradykinin inhibitory peptidase [1].

Bradykinin Potentiator C, a potent inhibitor of angiotensin-converting enzyme (ACE) with an inhibitory concentration (IC 50) of 7.1 μM for rabbit lung ACE, is regarded as a prototype for functional peptides [1].

Compound 2, known as KCC2 potentiators-1, acts as an enhancer of the potassium chloride cotransporter-2 (KCC2). It holds potential for applications in studies related to neurological disorders.

Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP). Chromenone 1 induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.

LY450108 is a potentiator of the AMPA receptor that can be used in Parkinson's disease studies.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Ivacaftor (VX-770) (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively.

PG01 is a potent CFTR Cl-channel potentiator, effective against ΔF508 (Ka 0.3 μM), and also against E193K, G970R and G551D (CFTR mutants), with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively.PG01 increases ΔF508-CFTR Cl- currents upon addition of forskolin. F508-CFTR Cl-current upon addition of Forskolin, correcting the gating defect of CFTR mutants.

VU0152099 is a potent and selective M4 mAChR allosteric potentiator(EC50 = 380 ± 93 nM).

GLPG1837 (ABBV-974) is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

Cinepazide is a vasodilator used for the treatment of cardiovascular, cerebrovascular, and peripheral vascular diseases. Cinepazide acts as a potentiator of adenosine A2 receptors.

Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons.

GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator that effectively enhances the function of low-temperature-rescued F508del CFTR with an EC50 of 11.1 nM.

Ivacaftor benzenesulfonate, used for cystic fibrosis treatment, is an orally bioavailable CFTR potentiator.

Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.

Biphenylindanone A is a selective potentiator of human mGluR2 (hmGluR2),and for the treatment of neurological disorders.

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit, with EC50 values of 2.7 μM for NR2C and 2.8 μM for NR2D.

Mibampator (LY451395) is an effective and selective AMPA receptor potentiator.

VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).