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σ2-receptor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111669
    CT1812
    1 Publications Verification

    Sigma-2 receptor antagonist 1

    		 Sigma Receptor Neurological Disease
    CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease .
    CT1812
  • HY-B1813A
    (±)-Vesamicol hydrochloride

    (±)-AH5183 hydrochloride

    		 Sigma Receptor Neurological Disease
    (±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively [2].
    (±)-Vesamicol hydrochloride
  • HY-14221A
    Siramesine hydrochloride
    4 Publications Verification

    Lu 28-179 hydrochloride

    		 Sigma Receptor Ferroptosis Cancer
    Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity [2] .
    Siramesine hydrochloride
  • HY-14221
    Siramesine

    Lu 28-179

    		 Sigma Receptor Cancer
    Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity [2] .
    Siramesine
  • HY-14221B
    Siramesine fumarate

    LU-28-179 fumarate

    		 Sigma Receptor Cancer
    Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity [2] .
    Siramesine fumarate
  • HY-14218
    Ditolylguanidine
    2 Publications Verification

    1,3-Di-o-tolylguanidine; DTG

    		 Sigma Receptor Neurological Disease
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer [2] .
    Ditolylguanidine
  • HY-163075
    SYB4

    		Others Others
    SYB4 (compound 5) is a PET tracer which suitable for imaging the Sigma-2 Receptor in the brain of nonhuman primates .
    SYB4
  • HY-B2087
    Glycerol phenylbutyrate

    HPN-100
    Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent [2].
    Glycerol phenylbutyrate
  • HY-100155
    4-IBP

    		Sigma Receptor Cancer
    4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).
    4-IBP
  • HY-125819
    Sigma-1 receptor antagonist 2

    		Sigma Receptor Neurological Disease
    Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively .
    Sigma-1 <em>receptor</em> antagonist <em>2</em>
  • HY-151562
    AChE/BuChE/MAO-B-IN-1

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research .
    AChE/BuChE/MAO-B-IN-1
  • HY-14813
    Cutamesine

    SA4503; AGY 94806

    		 Sigma Receptor Neurological Disease
    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
    Cutamesine
  • HY-155616
    KSK94

    		Sigma Receptor Histamine Receptor Neurological Disease
    KSK94 is a high-affinity histamine H3 receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .
    KSK94
  • HY-19469
    Roluperidone
    1 Publications Verification

    CYR-101; MIN-101; MT-210

    		 5-HT Receptor Sigma Receptor Neurological Disease
    Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
    Roluperidone
  • HY-155615
    KSK67

    		Sigma Receptor Histamine Receptor Neurological Disease
    KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .
    KSK67
  • HY-122112
    CM572

    		Sigma Receptor Cancer
    CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
    CM572
  • HY-107708
    threo-Ifenprodil hemitartrate

    		iGluR Sigma Receptor Potassium Channel Neurological Disease
    threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity [2] .
    threo-Ifenprodil hemitartrate
  • HY-155614
    KSK68

    		Sigma Receptor Histamine Receptor Neurological Disease
    KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .
    KSK68
  • HY-155992
    WLB-89462

    		Sigma Receptor Neurological Disease
    WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
    WLB-89462
  • HY-145628
    CM398

    		Sigma Receptor Neurological Disease Inflammation/Immunology
    CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
    CM398
  • HY-108511A
    PB28

    		Sigma Receptor Apoptosis SARS-CoV Infection Cancer
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity [2] .
    PB28
  • HY-108511
    PB28 dihydrochloride

    		Sigma Receptor Apoptosis SARS-CoV Infection Cancer
    PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity [2] .
    PB28 dihydrochloride

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