2. Signaling Pathways
  3. Neuronal Signaling
  4. Sigma Receptor

Sigma Receptor

Sigma Receptor

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Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body. The endogenous ligand for these sites has not been identified, but steroid hormones (particularly progesterone), sphingolipid-derived amines and N,N-dimethyltryptamine can bind with fairly high affinity.

The sigma-1 receptor (σ1R) is an endoplasmic reticulum (ER)-resident chaperone protein that acts like an inter-organelle signaling modulator. It participates in many biological processes including nociception, cancer, stroke, memory, drug addiction, cardiac activity, and Alzheimer’s disease. The sigma-2 (σ2R) receptor is overexpressed in various human tumors. It has been validated as a biomarker for proliferating tumors.

Sigma Receptor Isoform Specific Products:

Sigma Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13575A
    Blonanserin dihydrochloride
    		Antagonist
    Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin dihydrochloride
  • HY-116586
    AF710B
    		Agonist
    AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.
    AF710B
  • HY-14221B
    Siramesine fumarate
    		Agonist
    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-163075
    SYB4
    SYB4 (compound 5) is a PET tracer which suitable for imaging the Sigma-2 Receptor in the brain of nonhuman primates.
    SYB4
  • HY-158197
    RC-106
    		Inhibitor
    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-149855
    AB10
    		Antagonist
    AB10 is a selective S1R antagonist. AB10 with Ki of 10, 165 nM for S1R and S2R, respectively. AB10 reverses the effect of Capsaicin (HY-10448) caused pain in model.
    AB10
  • HY-155616
    KSK94
    		Antagonist
    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-147560
    σ1 Receptor/μ Opioid receptor modulator 1
    		Antagonist
    σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain.
    σ1 Receptor/μ Opioid receptor modulator 1
  • HY-RS12910
    Sigmar1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Sigmar1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sigmar1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sigmar1 Rat Pre-designed siRNA Set A
    Sigmar1 Rat Pre-designed siRNA Set A
  • HY-121867
    KSCM-11
    KSCM-11 is a ligand of thesigma receptor.
    KSCM-11
  • HY-100930
    L-693403 maleate
    L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research.
    L-693403 maleate
  • HY-155155
    SARS-CoV-2-IN-57
    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-116586A
    (Rac)-AF710B
    		Agonist
    (Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.
    (Rac)-AF710B
  • HY-116463B
    (2S,3S)-E1R
    		Agonist 98.24%
    (2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
    (2S,3S)-E1R
  • HY-18100AR
    PRE-084 (hydrochloride) (Standard)
    		Agonist
    PRE-084 (hydrochloride) (Standard) is the analytical standard of PRE-084 (hydrochloride). This product is intended for research and analytical applications. PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
    PRE-084 (hydrochloride) (Standard)
  • HY-131914B
    EST64454 maleate
    		Antagonist
    EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
    EST64454 maleate
  • HY-155614
    KSK68
    		Antagonist
    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-149335
    Sigma-1 receptor antagonist 5
    		Antagonist
    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-155615
    KSK67
    		Antagonist
    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-163065
    σ1 Receptor/μ Opioid receptor modulator 2
    		Antagonist
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models.
    σ1 Receptor/μ Opioid receptor modulator 2
Sigma Receptor Isoform Comparison

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