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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V3950 | 4-IBP | 155798-08-6 | 4-IBP is a novel and selective σ1 (sigma1) agonist with high affinity for the σ1 receptor with Ki of 1.7 nM and a moderate affinity for the σ2 receptor (Ki = 25.2 nM). |
|
V79226 | AB10 | AB10 is a selective S1R antagonist. | |
|
V79240 | AB21 | AB21 is a potent and specific S1R antagonist (inhibitor) with Ki of 13 nM and 102 nM for S1R and S2R, respectively. | |
|
V78890 | AB21oxalate | AB21 oxalate is a potent and specific S1R antagonist (inhibitor) with Ki of 13 nM and 102 nM for S1R and S2R, respectively. | |
|
V79439 | AD186 | AD186 is a potent and specific S1R agonist/activator with Ki of 2.7 and 27 nM for S1R and S2R respectively. | |
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V80042 | Antidepressant agent 3 | Antidepressant agent 3 is an orally bioactive antidepressant. | |
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V77994 | Antidepressant agent 4 | Antidepressant agent 4 is an orally bioactive antidepressant. | |
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V2985 | BD 1047 dihydrobromide | 138356-21-5 | BD1047 dihydrobromide (BD-1047) is a selective functional antagonist of sigma receptors (σ receptors) with antipsychotic activity and may be used for schizophrenia. |
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V4741 | BD1063 HCl | 206996-13-6 | BD-1063 HCl (BD1063 hydrochloride) is a novel, potent and selective sigma receptor antagonist with the potential for treatingalcoholism. |
|
V71977 | Broussoflavonol F | 162558-94-3 | Broussoflavonol F has xanthine oxidase inhibitory activity. |
|
V70033 | CM398 | 1121931-70-1 | CM398 is a selective, orally bioactive sigma-2 receptor ligand (Ki=0.43 nM) with a high sigma-1/sigma -2 selectivity ratio (1000-fold). |
|
V3312 | CT-1812 | 1802632-22-9 | CT1812 (Elayta) is a novel, potent andorally bioavailable allosteric antagonist of the sigma-2 receptor complex (sigma-2/PGRMC1) that prevents and displaces binding of Aβ oligomers to neurons. |
|
V0097 | Cutamesine (SA 4503; AGY 94806) | 165377-43-5 | Cutamesine (SA-4503; AGY-94806) is a selective and potent sigma-1 (σ1) receptor agonist with an IC50of 17.4 nM in guinea pig brain membranes, 100-fold less selective for the sigma 2 receptor. |
|
V30747 | Dimemorfan phosphate | 36304-84-4 | Dimemorfan phosphate (Astomin; AT17; Gentus; AT-17) is a morphinan-based sigma 1 receptor agonistwith potent antitussive activity. |
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V70037 | DuP 734 | 135135-87-4 | DuP 734 is a sigma receptor antagonist. |
|
V2275 | EST64454 HCl | 1950569-11-5 | EST64454 HCl is a selective and orally bioactive sigma-1 receptor blocker (antagonist) with Ki of 22 nM. |
|
V69891 | EST73502 monohydrochloride | 2535970-65-9 | EST73502 mono HCl is a selective, orally bioactive, BBB (blood-brain barrier) permeable (penetrable) μ-opioid receptor (μ-opioid receptor/MOR) agonist and σ1 receptor (σ1R) antagonist, targeting MOR and σ1R The Kis of the effects are 64 nM and 118 nM respectively. |
|
V71980 | Eupatoriochromene | 19013-03-7 | Eupatoriochromene is a benzopyran compound with inhibitory activity against xanthine oxidase (XO). |
|
V71979 | Febuxostat-d9 (Febuxostat d9) | 1246819-50-0 | Febuxostat-d9 is the deuterium labelled form of Febuxostat. |
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V71976 | Forsythoside F (Forsythoside F; Arenarioside) | 94130-58-2 | Forsythoside F is a xanthine oxidase inhibitor that has anti-hyperuric acid effects. |
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