modulatory

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

Posatirelin (BRN6006446) is a synthetic peptide with modulatory activity and neurotrophic effects on monoaminergic and cholinergic systems for the study of vascular dementia.

DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of 3,3′-difluorobenzaldazine (DFB).

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

Agmatine sulfate (Agmatine sulfate salt) is a bioactive metabolite of the arginine amino acid. It exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

Thymulin is a peptide hormone which is mainly produced by thymic epithelial cells and it has immune-modulatory and anti-inflammatory effects

MRZ 2-514 (8-bromo-4,5-dihydroxypyridazino[4,5-b]quinolin-1-one) is a strychnine-insensitive modulatory site of the NMDA receptor (glycineB)antagonist with Ki of 33 μM.

Salicortin is a phenolic glycoside isolated from many plants such as Populus and Salix species, has anti-adipogenic, anti-amnesic, and immune-modulatory activity.

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

JNJ-46281222 is a metabotropic glutamate (mGlu) 2-selective, highly potent positive allosteric modulator (PAM) with nanomolar affinity (Kd = 1.7 nM) and high modulatory potency (pEC50 = 7.71).

BMS-986169 is a GluN2B Receptor Negative Allosteric Modulator. BMS-986169 showed a high binding affinity for the GluN2B subunit allosteric modulatory site (Ki: 4.03-6.3 nM) and selectively inhibited GluN2B receptor function in Xenopus oocytes expressing h

Glaspimod is a synthetic hematoregulatory peptide. It shares biological and/or modulatory activities with natural hematopoetic cytokines.

GW-Amide is a molluscan neuropeptide that exhibits potent modulatory effects on molluscan muscles.

ACT-1004-1239 is an orally active, selective, and potent CXCR7 antagonist with immune-modulatory and myelin-promoting effects. It can be used to study inflammatory demyelinating diseases.

Theaflavin digallate and lactic acid together could reduce herpes simplex virus transmission.

KA2507 hydrochloride is a powerful and specific HDAC6 inhibitor, possessing an IC50 value of 2.5 nM. It displays no substantial toxicities while demonstrating significant antitumor efficacy and immune modulatory effects [1].

DM175 is a novel partial FXR agonist, causing specific modulatory effects on FXR activity that clearly differ from classical FXR agonists.

Flupirtine HCl is the salt form of Flupirtine, also known as W-2964, an aminopyridine that functions as a centrally acting non-opioid analgesic. It first became available in Europe in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Like nefopam, it is unique among analgesics in that it is a non-opioid, non-NSAID, non-steroidal centrally acting analgesic. Flupirtine is a selective neuronal potassium channel opener that also has NMDA receptor antagonist and GABAA receptor modulatory properties.

Keap1-Nrf2-IN-9 (compound 11) is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI) with an IC50 value of 0.575 µM, enhancing the expression of Nrf2 target genes such as heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and glutamate-cysteine ligase catalytic (Gclc) and modulatory (Gclm) subunits, while not being cytotoxic to ARPE19 cells [1].

Tamuzimod, an effective immunomodulator, exhibits modulatory activity on S1P Receptors with EC50 values below 1 μM [1] [2].

JWH 030 is a potent naphthoyl pyrrole cannabimimetic, exhibiting higher affinity for the CB1 receptor (EC50= 30.5 nM in rats, Ki= 87 nM in mice) compared to CB2 (EC50= 552 nM in human CB2 receptors). The compound demonstrates significant in vivo potency in mouse models, specifically in spontaneous activity and tail flick assays (antinociception) with an ED50 value of 26.8 μM/kg. Furthermore, JWH 030 dose-dependently reduces electrically-induced contractions in the mouse vas deferens, with an IC50 of 3.38 nM, highlighting its effective modulatory effects. This compound is designated for forensic or research applications.

Desethoxy quetiapine, an active metabolite of the atypical antipsychotic quetiapine, primarily forms through the action of the cytochrome P450 (CYP) isoform CYP3A5. This compound binds to dopamine D2 receptors with an IC50 value of 1,330 nM. In vivo, desethoxy quetiapine at dosages of 20 and 40 mg kg mitigates dopamine receptor agonist apomorphine-induced climbing behavior and ameliorates swimming deficits in mice, showcasing its potential modulatory effects on dopamine-mediated behaviors.

The synthetic caged Garcinia xanthone cluvenone induces cell stress and apoptosis and has immune modulatory activity.