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Isoforms Recommended: Sigma 2 Receptor
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sigma-2 receptor

" in MedChemExpress (MCE) Product Catalog:
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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-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 .
    Siramesine hydrochloride
  • 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-B2087
    Glycerol phenylbutyrate

    HPN-100

    		 Sigma Receptor Cardiovascular Disease
    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 .
    Glycerol phenylbutyrate
  • 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-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 .
    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 .
    Siramesine fumarate
  • 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-163075
    SYB4

    		Sigma Receptor Others
    SYB4 (compound 5) is a PET tracer which suitable for imaging the Sigma-2 Receptor in the brain of nonhuman primates .
    SYB4
  • HY-135608
    BD-1008

    		Others Others
    BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.
    BD-1008
  • HY-169185
    Sigma-2 Radioligand 2

    		Sigma Receptor Cancer
    Sigma-2 Radioligand 2 (compund 4) exhibits low nanomolar affinity (Ki(σ2)=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor .
    Sigma-2 Radioligand 2
  • HY-117420
    CM764

    		Sigma Receptor Cancer
    CM764 is an activator for sigma receptor with Ki of 86.6 and 3.5 nM for sigma-1 receptor and sigma-2 receptor. CM764 increases cytoplasmic calcium, NAD +/NADH, and ATP levels, and decreases the concentration of ROS .
    CM764
  • HY-B2087R
    Glycerol phenylbutyrate (Standard)

    		Sigma Receptor Cardiovascular Disease
    Glycerol phenylbutyrate (Standard) is the analytical standard of Glycerol phenylbutyrate. This product is intended for research and analytical applications. 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 .
    Glycerol phenylbutyrate (Standard)
  • 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-118279
    KSCM-1

    		Sigma Receptor Neurological Disease
    KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors .
    KSCM-1
  • 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-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-120421
    SW116 free base

    		Sigma Receptor Cancer
    SW116 free base is a selective fluorescent ligand for sigma-2 receptor with a Ki of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research .
    SW116 free base
  • HY-14222
    UMB24

    		Sigma Receptor Neurological Disease
    UMB24 is a potent antagonist of σ2 receptor, with Ki values of 170 nM anf 322 nM for σ2 receptor and σ1 receptor, respectively. UMB24 attenuats cocaine-induced convulsions and locomotor activity, but not lethality .
    UMB24
  • 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 .
    Ditolylguanidine
  • 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 receptor antagonist 2
  • 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-108513
    σ1 Receptor antagonist 4

    		Sigma Receptor Neurological Disease
    σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .
    σ1 Receptor antagonist 4
  • 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 .
    (±)-Vesamicol hydrochloride
  • 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-101376
    (+)-N-Allylnormetazocine hydrochloride

    (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride

    		 Opioid Receptor Neurological Disease
    (+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease .
    (+)-N-Allylnormetazocine hydrochloride
  • 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 .
    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 .
    PB28 dihydrochloride
  • HY-108512
    PD 144418
    1 Publications Verification

    		 Sigma Receptor Neurological Disease
    PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity .
    PD 144418
  • 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 .
    threo-Ifenprodil hemitartrate
  • HY-108512A
    PD 144418 oxalate
    1 Publications Verification

    		 Sigma Receptor Neurological Disease
    PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity .
    PD 144418 oxalate
  • HY-117731
    UKH-1114

    		Sigma Receptor Neurological Disease
    UKH-1114 is a potent σ2 receptor/Tmem97 agonist with a Ki value of 46 nM, showing antimechanical hypersensitivity effects. UKH-1114 alleviates mechanical hypersensitivity caused by nerve injury without any movement disorders in mice. UKH-1114 is promising for research of neuropathic pain .
    UKH-1114
  • HY-149335
    Sigma-1 receptor antagonist 5

    		Sigma Receptor Histamine Receptor Neurological Disease
    Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models .
    Sigma-1 receptor antagonist 5
  • HY-18099A
    S1RA hydrochloride
    1 Publications Verification

    E-52862 hydrochloride

    		 Sigma Receptor 5-HT Receptor Neurological Disease
    S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
    S1RA hydrochloride
  • 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-134004
    Pentoxyverine

    Carbetapentane

    		 Sigma Receptor mAChR Neurological Disease Inflammation/Immunology
    Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
    Pentoxyverine
  • HY-B1055
    Pentoxyverine citrate

    Carbetapentane citrate

    		 Sigma Receptor mAChR Neurological Disease Inflammation/Immunology
    Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
    Pentoxyverine citrate
  • HY-134004R
    Pentoxyverine (Standard)

    		Sigma Receptor mAChR Neurological Disease Inflammation/Immunology
    Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
    Pentoxyverine (Standard)
  • HY-B1055R
    Pentoxyverine (citrate) (Standard)

    		Sigma Receptor mAChR Neurological Disease Inflammation/Immunology
    Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].
    Pentoxyverine (citrate) (Standard)

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