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-176405
    σ1R-IN-1
    		Inhibitor
    σ1R-IN-1 ((R,R)-1a) is a potent σ-1R inhibitor with an IC50 of 110 nM. σ1R-IN-1 is promising for research of neuropsychiatric disorders.
    σ1R-IN-1
  • HY-122224
    SW43
    		Agonist
    SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA (89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis.
    SW43
  • HY-116463D
    (Rac)-E1R
    		Agonist 98.48%
    (Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.
    (Rac)-E1R
  • HY-129485A
    CM304 free base
    		Antagonist
    CM304 free base (FTC-146) is a potent S1R antagonist. CM304 free base enhances the antinociceptive effects of the cannabinoid receptor agonists. CM304 free base inhibits convulsions in rats.
    CM304 free base
  • HY-151951
    Antidepressant agent 4
    Antidepressant agent 4 is an orally active antidepressant agent. Antidepressant agent 4 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 4
  • HY-107047
    BGC-201259
    		Inhibitor
    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-116463A
    (2R,3S)-E1R
    		Agonist 98.84%
    (2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
    (2R,3S)-E1R
  • HY-177345
    SV119
    		Ligand
    SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer.
    SV119
  • HY-RS12908
    SIGMAR1 Human Pre-designed siRNA Set A
    		Inhibitor

    SIGMAR1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIGMAR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SIGMAR1 Human Pre-designed siRNA Set A
  • HY-161873
    PW507
    		Antagonist
    PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN).
    PW507
  • HY-117420
    CM764
    		Activator
    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-120008
    SAS-1121
    		Ligand
    SAS-1121 is a subtype-selective sigma 2 receptor/PGRMC1 ligand with a Ki of 16.2 nM. SAS-1121 is 574-fold selective for the signma 2 receptor over the sigma 1 receptor. SAS-1121 is a tertiary amine. SAS-1121 can be studied in neurology-related research.
    SAS-1121
  • HY-149854A
    AB21 oxalate
    		Antagonist
    AB21 oxalate is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity.
    AB21 oxalate
  • HY-116463C
    (2R,3R)-E1R
    		Agonist 98.79%
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
    (2R,3R)-E1R
  • HY-118901A
    Opipramol dihydrochloride
    		Antagonist
    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-120360
    CB-64D
    		Agonist
    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-119196
    Caprospinol
    		Ligand
    Caprospinol (SP-233) is a steroid compound candidate based on the structure of 22R-hydroxycholesterol. It has multiple mechanisms of neuroprotection, including binding to β-amyloid protein (Aβ(42)), interacting with the mitochondrial respiratory chain, clearing Aβ(42) monomers, and acting as a σ-1 receptor ligand. It can cross the blood-brain barrier in vivo and restore cognitive impairment, and has the potential to inhibit Alzheimer's disease.
    Caprospinol
  • HY-106153B
    E-5842 citrate
    		Ligand
    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-149854
    AB21
    		Antagonist
    AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 has the effect of reducing mechanical hypersensitivity.
    AB21
  • HY-151950
    Antidepressant agent 3
    Antidepressant agent 3 is an orally active antidepressant agent. Antidepressant agent 3 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 3
Sigma Receptor Isoform Comparison

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