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. |
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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. |
|
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. |
|
V94242 | EST64454 | 1351438-26-0 | EST64454 (Compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki of 22 nM. |
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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. |
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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. |
|
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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V93033 | UMB24 | 1033-69-8 | UMB24 is a potent σ2 receptor antagonist with Ki values of 170 nM and 322 nM for σ2 and σ1 receptors, respectively. |
|
V87842 | WLB-87848 | 2839205-09-1 | WLB-87848 is a selective, orally active, blood-brain-penetrating σ1 receptor agonist with a Ki value of 9 nM. |
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V87844 | σ1 Receptor antagonist 4 | 362512-81-0 | σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with Ki of 10 nM. |
|
V93252 | σ1 Receptor ligand 1 | σ1 receptor ligand 1 (Compound 5I) is a σ1 receptor ligand with Ki value of 3.9 nM. |
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