The entire mammalian body expresses a special class of binding sites known as sigma receptors (subtypes sigma-1 and sigma-2). Although the endogenous ligand for these sites has not been discovered, N,N-dimethyltryptamine, sphingolipid-derived amines, and steroid hormones—especially progesterone—can bind with a fair amount of affinity.
The sigma-1 receptor (1R) is a chaperone protein that resides in the endoplasmic reticulum (ER) and functions as a modulator of inter-organelle signaling. Numerous biological processes, such as nociception, cancer, stroke, memory, drug addiction, cardiac activity, and Alzheimer's disease, are affected by it. Numerous human tumors have an overexpression of the sigma-2 (2R) receptor. It has been proven to be a reliable biomarker for spreading tumors.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2044 | S1RA HCl (E-52862) | 1265917-14-3 | S1RA HCl (also known as E-52862 HCl) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM). |
|
V2813 | SA4503 dihydrochloride | 165377-44-6 | SA4503 dihydrochloride (also known asAGY94806 dihydrochloride andCutamesine dihydrochloride), is a potent sigma-1 (σ1) receptor agonist with an IC50of 17.4 nM in guinea pig brain membranes. |
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V79463 | Sigma-1 receptor antagonist 4 | Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effects of morphine and rescues morphine-induced analgesic tolerance, with the potential to prevent morphine tolerance. | |
|
V78792 | Sigma-1 receptor antagonist 5 | Sigma-1 receptor antagonist 5 (compound 12) is a 4-pyridine analogue with analgesic activity and a sigma receptor (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and histamine H3 (hH3R, Ki= 7.7 nM, IC50=215 nM) antagonist. | |
|
V70046 | Sigma-2 Radioligand 1 | 2860554-32-9 | Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. |
|
V3703 | Siramesine | 147817-50-3 | Siramesine (Formerly known as Lu-28-179) is a potent and selective agonist of sigma-2 receptor. |
|
V2908 | Siramesine HCl | 224177-60-0 | Formerly known as Lu-28-179, siramesine HCl is a potent and selective sigma-2 receptor agonist with anticancer effects. |
|
V86295 | SOMCL-668 | 1422251-09-9 | |
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V71970 | Tetrahydroamentoflavone (Amentoflavone) | 48236-96-0 | Tetrahydroamentoflavanone (Amentoflavanone) is a potent xanthine oxidase (XO) inhibitor. |
|
V71968 | Tigulixostat (LC350189) | 1287766-55-5 | Tigulixostat (LC350189) is an orally bioactive, non-purine-selective xanthine oxidase inhibitor. |
|
V27982 | Vesamicol hydrochloride, (+/-)- | 120447-62-3 | (±)-Vesamicol HCl ((±)-AH5183 HCl) is a potent inhibitor of vesicular acetylcholine transport with Ki of 2 nM. |
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V70039 | WLB-89462 | 2849471-75-4 | WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). |
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V71971 | Xanthine oxidase-IN-10 | 851429-65-7 | Xanthine oxidase-IN-10 (XO8 analog) is a xanthine oxidase (XO) inhibitor. |
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V71986 | Xanthine oxidoreductase-IN-3 | 651769-78-7 | Xanthine oxidoreductase-IN-3 is an orally bioactive xanthine oxidoreductase (XOR) inhibitor (antagonist) with IC50 of 26.3 nM. |
|
V70031 | σ1 Receptor antagonist-1 | 1204401-49-9 | σ1 Receptor antagonist-1 is a highly efficient and selective sigma 1 receptor antagonist (pKi=10.28). |
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