polarization

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

IMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.IMP-1710 has antifibrotic activity. [1]

γ-Aminobutyric acid (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

Mepivacaine hydrochloride (Mepivacaine HCl) is the hydrochloride salt form of mepivacaine, an amide derivative with local anesthetic properties.

Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.

Ivabradine hydrochloride (S 16257-2) is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization.

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group. It is employed across various applications for controlling a wide array of pests. As a neurotoxin, λ-Cyhalothrin acts on sodium channels in neuron membranes within the central nervous system.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

(Z)-Leukadherin-1 (ADH-503 free base) is an allosteric agonist of CD11b.

ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 is a potent and orally active KCNQ2/Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects.

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

(RS)-AMPA ((±)-AMPA) is a glutamate analog and an agonist of the effective and selective excitatory neurotransmitter L-glutamic acid.

Alosetron hydrochloride (GR 68755) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system, particularly on enteric and nociceptive sensory neurons, thereby affecting the regulation of visceral pain, decreasing gastrointestinal contraction and motility, and decreasing gastrointestinal secretions.

VU0071063 is a Kir6.2/SUR1 activator.

ZD7288 (ICI D7288), a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity.

ADH-503 (GB1275) is an orally available, allosteric CD11b small molecule agonist that can lead to repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhancement of dendritic cell responses.

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a) (IC50=5-20 nM). Etomoxir inhibits fatty acid oxidation by inhibiting CPT-1a, inhibits palmitate oxidation, has an inhibitory effect on adenine nucleotide translocase, and can inhibit macrophage polarization by disrupting CoA homeostasis.

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

L-Methionine sulfoxide (H-Met(O)-OH) is a metabolite of Methionine that modulates oxidative stress and purinergic signaling parameters, while inducing M1/classical macrophage polarization.

Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a corticosteroid with anti-inflammatory properties that promotes the polarization of M1 to M2 macrophages by reducing the secretion of pro-inflammatory cytokines, and is utilized in research on keloids and rheumatoid arthritis.

Neotuberostemonine (NTS) is one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, it has a significant protective effect on bleomycin (BLM)-induced pulmonary fibrosis through suppressing the recruitment and M2 polarization of macroph

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

Anti-MRSA agent 18 (E17) is an inhibitor of MRSA, exhibiting MIC values of 2 μg/mL for S. aureus and 4 μg/mL for MRSA. This compound accelerates bacterial death by interacting with the bacterial cell membrane constituents, phosphatidylglycerol and cardiolipin, leading to changes in membrane permeability and polarization. Additionally, it increases intracellular ROS, along with leakage of DNA and proteins.

Neuroprotective agent 5 (compound 28) acts as a brain-penetrating agent with anti-neuroinflammatory, antioxidant, and neuroprotective properties. It exhibits potent inhibition of nitric oxide (NO) with an EC50 of 0.49 μM and suppresses the release of pro-inflammatory mediators PGE2 and TNF-α. Additionally, it downregulates the expression of iNOS and COX-2 proteins, facilitating the polarization of BV-2 cells from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype. Neuroprotective agent 5 also dose-dependently inhibits acetylcholinesterase (AChE) activity and the aggregation of Aβ42. This compound is useful for research into Alzheimer's disease.