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-149803
    S1R agonist 1
    		Agonist ≥98.0%
    S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
    S1R agonist 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
  • HY-47228
    KB-5492 free base
    		Inhibitor 99.02%
    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-149803A
    S1R agonist 1 hydrochloride
    		Agonist 99.83%
    S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
    S1R agonist 1 hydrochloride
  • HY-19120
    KB-5492 anhydrous
    		Inhibitor 99.50%
    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-169914
    Igmesine hydrochloride
    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-125820
    Sigma-1 receptor antagonist 3
    		Antagonist 99.47%
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain.
    Sigma-1 receptor antagonist 3
  • HY-108515
    (+)-Igmesine hydrochloride
    		Ligand 99.0%
    (+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ1 receptor ligand with an IC50 of 39 nM. (+)-Igmesine hydrochloride binds σ1 receptors to activate G-proteins and modulate Ca2+ uptake. (+)-Igmesine (hydrochloride) attenuates ischaemia-induced nitric oxide synthase activity and hyperactivity. (+)-Igmesine hydrochloride can be used for the research of duodenal ulcers, gastric ulcers, and cerebral ischaemia.
    (+)-Igmesine hydrochloride
  • HY-125819
    Sigma-1 receptor antagonist 2
    		Antagonist 99.76%
    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-RS12909
    Sigmar1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sigmar1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sigmar1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sigmar1 Mouse Pre-designed siRNA Set A
  • HY-116594
    OPC-14523 free base
    		Agonist
    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-100966
    BD-1008 dihydrobromide
    		Antagonist 98.07%
    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-134189A
    EST73502 monohydrochloride
    		Antagonist 99.58%
    EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.
    EST73502 monohydrochloride
  • HY-117731
    UKH-1114
    		Agonist 99.88%
    UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a Ki values of 1279 and 46 nM for σ1R and σ2R/TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research.
    UKH-1114
  • HY-101626
    Sigma ligand-1
    		99.67%
    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-149804
    S1R agonist 2
    		Agonist ≥98.0%
    S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
    S1R agonist 2
  • HY-13751A
    SR-31747 free base
    SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
    SR-31747 free base
  • HY-14218R
    Ditolylguanidine (Standard)
    		Agonist
    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-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-100966S
    BD-1008-d5 dihydrobromide
    		Antagonist
    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-d<sub>5</sub> dihydrobromide
Sigma Receptor Isoform Comparison

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