Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body.Although the natural ligand for these sites is unknown, steroid hormones—especially progesterone—amines derived from sphingolipids, and N,N-dimethyltryptamine—all have a relatively high affinity for binding.
The sigma-1 receptor (σ1R) is a chaperone protein that resides in the endoplasmic reticulum (ER) and functions as an inter-organelle signaling modulator. Numerous biological processes are impacted by it, such as nociception, drug addiction, cardiac activity, cancer, stroke, memory, and Alzheimer's disease. Numerous human tumors exhibit overexpression of the sigma-2 (σ2R) receptor. Its status as a proliferating tumor biomarker has been confirmed.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V93275 | (±)-PPCC | 932736-90-8 | (±)-PPCC is a sigma-1 agonist that primarily interacts with the sigma-1 receptor with a Ki of 1.5 nM. |
|
V87843 | (±)-PPCC hemioxalate | 932736-91-9 | (±)-PPCC hemioxalate is a compound with sigma-1 receptor modulatory activity. |
|
V87845 | AB21 hydrochloride | 3026677-24-4 | AB21 hydrochloride is a potent and selective S1R antagonist with Ki values of 13 nM and 102 nM for S1R and S2R, respectively. |
|
V103727 | AD353 | AD353 is a selective sigma-1 receptor ligand. | |
|
V7110 | Anavex2-73 HCl | 195615-84-0 | Anavex2-73 (Anavex-273; AE-37) HCl is a novel and potent muscarinic/σ1 ( Sigma-1) ligand/agonist (IC50 = 860 nM) with therapeutic potential for treating Alzheimer's disease. |
|
V116166 | BS148 | 2162116-09-6 | BS148 is a selective σ-2 receptor (S2R) agonist with a Ki value of 20 nM. |
|
V108977 | CM304 free base | 1350296-21-7 | CM304 free base (FTC-146) is a potent S1R antagonist. |
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V94242 | EST64454 | 1351438-26-0 | EST64454 (Compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki of 22 nM. |
|
V116204 | MS-377 | 206862-30-8 | MS-377 is a selective, orally effective σ-1 receptor ligand (Ki = 73 nM), with a weak affinity for σ-2 receptors (Ki = 6900 nM), and no affinity for other receptors (including dopamine receptors, serotonin receptors, PCP receptors, glutamate receptors, γ-aminobutyric acid receptors, adenosine receptors, and adrenaline receptors) (Ki > 10 μM). |
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V102730 | Opipramol dihydrochloride | 909-39-7 | Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). |
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V89040 | PW507 | 2573850-59-4 | PW507 is a potent, blood-brain permeable and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. |
|
V87694 | RC-106 | 1346216-50-9 | RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. |
|
V110368 | S1R agonist/BChE-IN-1 | S1R agonist/BChE-IN-1 (compound 7c) is an S1R agonist (IC50: 19 nM) and a selective BChE inhibitor (IC50 for human BChE: 37 nM). | |
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V115296 | SAS-0132 | 2095551-89-4 | SAS-0132 is a selective, blood-brain barrier-crossing Sigma 2 receptor (Sig2R) antagonist (Ki: 90 nM). |
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V115989 | SAS-1121 | 2095551-67-8 | SAS-1121 is a subtype-selective α2 receptor/PGRMC1 ligand with a Ki value of 16.2 nM. |
|
V98949 | Sigma-1 receptor antagonist 6 | 1335032-28-4 | Sigma-1 receptor antagonist 6 (Compound 12) is a Sigma-1 receptor (σ1R) antagonist. |
|
V94603 | Sigma-2 Radioligand 2 | 2860554-31-8 | Sigma-2 radioligand 2 (compound 4) exhibits low nanomolar affinity (Ki=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor. |
|
V118864 | SV119 | 913815-82-4 | SV119 is a selective σ₂ receptor ligand (Ki ≈ 5-10 nM). |
|
V113991 | SV119 hydrochloride | 913816-12-3 | SV119 hydrochloride is a σ² ligand with a Ki value of 5.2 nM. |
|
V101107 | SW116 free base | 1036759-00-8 | SW116 free base is a selective fluorescent ligand for sigma-2 receptor with Ki of 14 nM. |
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