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Sigma+Receptor

" in MedChemExpress (MCE) Product Catalog:

45

Inhibitors & Agonists

2

Biochemical Assay Reagents

2

Isotope-Labeled Compounds

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16996A
    BD-1047 dihydrobromide
    Maximum Cited Publications
    11 Publications Verification

    		 Sigma Receptor Neurological Disease
    BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .
    BD-1047 dihydrobromide
  • HY-118901
    Opipramol

    Ensidon; G-33040

    		 Sigma Receptor Neurological Disease
    Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
    Opipramol
  • HY-135608
    BD-1008

    		Sigma Receptor Neurological Disease
    BD-1008 is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor .
    BD-1008
  • HY-90002
    4-Phenylpiperidine

    		Sigma Receptor Neurological Disease
    4-Phenylpiperidine is a σ receptor ligand with a Ki value of 1980 nM for guinea pig σ receptors. 4-Phenylpiperidine binds to σ receptors. 4-Phenylpiperidine is used in psychiatric disease research .
    4-Phenylpiperidine
  • 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-108510
    Rimcazole dihydrochloride

    BW 234U dihydrochloride

    		 Sigma Receptor Dopamine Receptor Neurological Disease Cancer
    Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer .
    Rimcazole dihydrochloride
  • HY-155887
    DSPE-PEG-Amine, MW 3400 ammonium

    DSPE-PEG-NH2, MW 3400 ammonium

    		 Liposome Cancer
    DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
    DSPE-PEG-Amine, MW 3400 ammonium
  • HY-136280
    Panamesine

    EMD 57445

    		 Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-116594A
    OPC-14523 hydrochloride

    		Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .
    OPC-14523 hydrochloride
  • HY-136281
    DuP 734

    		Sigma Receptor Neurological Disease
    DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics .
    DuP 734
  • HY-169914
    Igmesine hydrochloride

    JO 1784 hydrochloride

    		 Sigma Receptor Neurological Disease
    Igmesine hydrochloride (JO 1784) is an orally active σ-receptor ligand capable of blocking the increase in colonic electromechanical activity induced by emotional stress. Igmesine hydrochloride also eliminates the colonic motility stimulation induced by dopamine, as well as the stimulation induced by centrally injected D1 or D2 receptor agonists. Furthermore, Igmesine hydrochloride can block the colonic motility responses induced by corticotropin-releasing factor (CRF) and ES through central cholecystokinin (CCK) release and/or activation of supraspinal CCK pathways .
    Igmesine hydrochloride
  • HY-47228
    KB-5492 free base

    		Sigma Receptor Inflammation/Immunology
    KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent .
    KB-5492 free base
  • HY-100966
    BD-1008 dihydrobromide

    		Sigma Receptor Neurological Disease
    BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .
    BD-1008 dihydrobromide
  • HY-107047
    BGC-201259

    RS-1259

    		 Cholinesterase (ChE) Serotonin Transporter 5-HT Receptor Calcium Channel Sodium Channel Sigma Receptor Neurological Disease
    BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease .
    BGC-201259
  • HY-A0139
    Thiothixene

    NSC 108165; Navan; Navane

    		 Sigma Receptor mAChR Histamine Receptor Dopamine Receptor Adrenergic Receptor Others
    Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    Thiothixene
  • HY-173475
    CM699

    		Sigma Receptor Dopamine Transporter Neurological Disease
    CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively .
    CM699
  • HY-120360
    CB-64D

    		Sigma Receptor Apoptosis Cancer
    CB-64D is the agonist for sigma receptor 2 and sigma receptor 1 with Ki of 16.5 and 3063 nM. CB-64D induces apoptosis in cancer cell SK-N-SH .
    CB-64D
  • HY-130179
    RC-33 hydrochloride

    		Apoptosis Neurological Disease
    RC-33 hydrochloride is a selective and metabolically stable σ receptor agonist with activity in enhancing nerve growth factor (NGF)-induced neurite outgrowth. Both enantiomers of RC-33 hydrochloride bind to the σ receptor with similar affinity and show almost equal effectiveness as σ receptor agonists. The R-configured enantiomer of RC-33 hydrochloride shows higher liver metabolic stability in the presence of NADPH. RC-33 hydrochloride was selected as the best candidate for further in vivo studies in animal models of amyotrophic lateral sclerosis .
    RC-33 hydrochloride
  • HY-120236
    KSCM-5

    		Sigma Receptor Neurological Disease
    KSCM-5 is a sigma receptor ligand with high affinity activity on sigma-1 receptor. The Ki value of KSCM-5 is about 34nM, showing significant selectivity. KSCM-5 has potential application value in compound development, especially for diseases related to sigma receptors .
    KSCM-5
  • HY-19120
    KB-5492 anhydrous

    		Sigma Receptor Inflammation/Immunology
    KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent .
    KB-5492 anhydrous
  • HY-121470
    Vesamicol

    AH5183

    		 Others Others
    Vesamicol is a compound used to synthesize radiolabeled derivatives that can be used as sigma receptor ligands for tumor targeting inhibition and have shown certain potential in cellular uptake, biodistribution and inhibition experiments.
    Vesamicol
  • HY-16996
    BD-1047

    		Sigma Receptor Neurological Disease
    BD-1047 is a selective functional antagonist of sigma receptors. BD-1047 attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .
    BD-1047
  • HY-158197
    RC-106

    		Sigma Receptor Proteasome Cancer
    RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM) .
    RC-106
  • HY-101626A
    Sigma ligand-1 hydrochloride

    		Sigma Receptor Neurological Disease
    Sigma ligand-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor .
    Sigma ligand-1 hydrochloride
  • HY-101626
    Sigma ligand-1

    		Sigma Receptor Neurological Disease
    Sigma ligand-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 has a Ki of 4000 nM at the dopamine D2 receptor .
    Sigma ligand-1
  • HY-118901A
    Opipramol dihydrochloride

    Ensidon dihydrochloride; G-33040 dihydrochloride

    		 Sigma Receptor Neurological Disease
    Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
    Opipramol dihydrochloride
  • 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-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-106153B
    E-5842 citrate

    		Sigma Receptor Neurological Disease
    E-5842 citrate is a σ receptor ligand (Ki: 4 nM for σ1 receptor). E-5842 citrate increases levels of Fos in the medial prefrontal cortex and the nucleus accumbens, without affecting the levels of the protein in the striatum. E-5842 citrate can be used in the research of psychiatric disorders .
    E-5842 citrate
  • HY-108509
    BMY-14802 hydrochloride

    BMY-14802-1; BMS 181100 hydrochloride

    		 Sigma Receptor 5-HT Receptor Adrenergic Receptor Neurological Disease
    BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects .
    BMY-14802 hydrochloride
  • HY-118901R
    Opipramol (Standard)

    Ensidon (Standard); G-33040 (Standard)

    		 Reference Standards Sigma Receptor Neurological Disease
    Opipramol (Standard) is the analytical standard of Opipramol. This product is intended for research and analytical applications. Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
    Opipramol (Standard)
  • HY-100966S
    BD-1008-d5 dihydrobromide

    		Isotope-Labeled Compounds Sigma Receptor Neurological Disease
    BD-1008-d5 dihydrobromide is the deuterium labeled BD-1008 dihydrobromide (HY-100966). BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .
    BD-1008-d5 dihydrobromide
  • HY-16996AR
    BD-1047 dihydrobromide (Standard)

    		Sigma Receptor Neurological Disease
    BD-1047 (dihydrobromide) (Standard) is the analytical standard of BD-1047 (dihydrobromide). This product is intended for research and analytical applications. BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .
    BD-1047 dihydrobromide (Standard)
  • HY-155155
    SARS-CoV-2-IN-57

    		SARS-CoV Sigma Receptor Infection
    SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC50: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively .
    SARS-CoV-2-IN-57
  • HY-105034
    Tiospirone

    BMY 13859-1 free base

    		 5-HT Receptor Neurological Disease
    Tiospirone is a 5-HT2 receptor antagonist with affinity for D2, 5-HT1a, and 5-HT7, and sigma receptors. Tiospirone decreases consumption of ethanol while increasing food intake of rats. Tiospirone can also reduce the reinforcing properties of Cocaine exhibited in the conditioned place preference paradigm .
    Tiospirone
  • HY-W714837
    5-Phenyllevulinic acid

    4-Oxo-5-phenylpentanoic acid; 5-Phenyl-4-oxopentanoic acid

    		 Bacterial Fungal Antibiotic Drug Intermediate Endogenous Metabolite Sigma Receptor Infection
    5-Phenyllevulinic acid (4-Oxo-5-phenylpentanoic acid) is an endogenous fungal metabolite with inhibitory activity against the bacterium B. megaterium, the plant pathogenic fungus S. tritici, and the alga C. fusca. 5-Phenyllevulinic acid is also an intermediate in the synthesis of σ receptor ligands. 5-Phenyllevulinic acid holds potential for research in the field of anti-infection studies .
    5-Phenyllevulinic acid
  • 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-14218R
    Ditolylguanidine (Standard)

    1,3-Di-o-tolylguanidine (Standard); DTG (Standard)

    		 Sigma Receptor Reference Standards Neurological Disease
    Ditolylguanidine (Standard) is the analytical standard of Ditolylguanidine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-116594
    OPC-14523 free base

    		Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity .
    OPC-14523 free base
  • 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-W748758
    (Z)-Thiothixene-d8

    NSC 108165-d8; Navan-d8; Navane-d8

    		 Isotope-Labeled Compounds Dopamine Receptor Histamine Receptor mAChR Adrenergic Receptor Sigma Receptor Others
    (Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    (Z)-Thiothixene-d8
  • HY-101626R
    Sigma ligand-1 (Standard)

    		Sigma Receptor Reference Standards Neurological Disease
    Sigma ligand-1 (Standard) is the analytical standard of Sigma ligand-1 (HY-101626). This product is intended for research and analytical applications. Sigma ligand-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 has a Ki of 4000 nM at the dopamine D2 receptor .
    Sigma ligand-1 (Standard)
  • HY-101626AR
    Sigma ligand-1 hydrochloride (Standard)

    		Sigma Receptor Reference Standards Neurological Disease
    Sigma ligand-1 (hydrochloride) (Standard) is the analytical standard of Sigma ligand-1 (hydrochloride) (HY-101626A). This product is intended for research and analytical applications. Sigma ligand-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor .
    Sigma ligand-1 hydrochloride (Standard)
  • HY-108510R
    Rimcazole dihydrochloride (Standard)

    BW 234U dihydrochloride (Standard)

    		 Reference Standards Sigma Receptor Dopamine Receptor Neurological Disease Cancer
    Rimcazole dihydrochloride (Standard) is the analytical standard of Rimcazole (dihydrochloride) (HY-108510). This product is intended for research and analytical applications. Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer .
    Rimcazole dihydrochloride (Standard)
  • HY-108509R
    BMY-14802 hydrochloride (Standard)

    BMY-14802-1 (Standard); BMS 181100 hydrochloride (Standard)

    		 Reference Standards Sigma Receptor 5-HT Receptor Adrenergic Receptor Neurological Disease
    BMY-14802 hydrochloride (Standard) is the analytical standard of BMY-14802 (hydrochloride) (HY-108509). This product is intended for research and analytical applications. BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects .
    BMY-14802 hydrochloride (Standard)

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