σ

RNAP-σ interaction inhibitor-2 (compound 7d) is an inhibitor targeting the interaction between RNA polymerase and the sigma factor. It demonstrates inhibitory activity against S. aureus with a minimum inhibitory concentration (MIC) of 2 µg/mL.

RNAP-σ interaction inhibitor-1 (compound 5d) acts as an inhibitor of the interaction between RNA polymerase and the sigma factor. It exhibits activity against Streptococci with a minimum inhibitory concentration (MIC) ranging from 1-2 µg/mL.

σ1 Receptor antagonist-1 is a selective σ1 receptor antagonist.

σ1R-IN-1 ((R,R)-1a) is an effective σ-1R inhibitor with an IC50 of 110 nM. It shows promising potential for use in research related to neuropsychiatric disorders.

σ 1 Receptor μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki value of 3.9 nM. It demonstrates a high plasma protein binding rate (89%) and exhibits good metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 is applicable in neuroscience and cancer research.

Compound 181, also known as 14-3-3σ ERα Stabilizer-1, is a covalent stabilizer targeting the 14-3-3σ ERα proteins. It is utilized in research as a molecular glue [1].

PTPσ Inhibitor ISP is a compound that binds to recombinant human PTPs, thereby inhibiting PTPσ signaling. It has the capability to penetrate membranes and counteract the inhibitory effects of chondroitin sulfate proteoglycan (CSPG) on axonal sprouting in spinal cord injury models. Additionally, it fosters remyelination in lysolecithin (LPC)-induced demyelinated spinal cords and supports the migration and maturation of oligodendrocyte progenitor cells (OPCs), enhancing remyelination and functional recovery in Multiple Sclerosis (MS) animal models [1] [2].

DJ001 is a highly specific, selective, and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with an IC50 of 1.43 μM, and it promotes the regeneration of hematopoietic stem cells.

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Sigma-LIGAND-1 is a selective Sigma Receptor ligand with IC50 values of 16 nM and 19 nM at the DTG site and the PPP site, respectively, and a Ki of 4000 nM at the dopamine D2 receptor.

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

Opipramol (Ensidon) is a compound with antidepressant activity that attenuates cocaine-seeking behavior in a rat model of self-administration.Opipramol is a sigma (σ) receptor agonist with anxiolytic activity and may be used in the study of neurological disorders.

KB-5492 free base is an orally available and selective antiulcer agent that inhibits sigma receptors, inhibits [3H]1,3-di(2-tolyl)guanidine (DTG) binding to sigma receptors, and may be useful in the study of gastric lesions and gastric secretion.

BD 1008 dihydrobromide is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM). BD 1008 dihydrobromide have high affinity for sigma1 receptors, moderate affinity for sigma2 receptors.

4-PPBP maleate is a potent σ1 receptor (ligand) agonist and a selective, non-competitive NR1a 2B NMDA receptor antagonist in the context of Xenopus oocytes expression, with neuroprotective properties.

BMY-14802 hydrochloride (BMS 181100 hydrochloride) is a selective antagonist of σ receptor (IC50 = 112 nM) with antipsychotic effects. BMY-14802 hydrochloride is an agonist of the α1-adrenergic receptor and 5-HT1A.

Sigma-1 receptor antagonist 1 is an effective and selective antagonist of sigma-1 receptor. Sigma-1 receptor antagonist 1 exhibits antineuropathic pain activity and can be used in the treatment of neuropathic pain studies.

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

BD1052 is a σ-receptor agonist known to intensify the behavioral toxicity of cocaine.

4-Hydroxy-1-(2-phenylethyl)piperidine is a synthetic ligand for muscarinic acetylcholine receptors (mAChR) or non-opioid intracellular sigma-1 receptors (σ1 receptors). It serves as a metabolite of the opioid compounds furanylfentanyl and 4-fluoroisobutyryl fentanyl (FIBF).

Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA) primarily functioning as a sigma (σ) receptor agonist. It interacts effectively with sigma recognition sites, having a Ki value of 50 nM. Opipramol is applicable in the study of generalized anxiety disorder (GAD).