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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V71979 | Febuxostat-d9 (Febuxostat d9) | 1246819-50-0 | Febuxostat-d9 is the deuterium labelled form of Febuxostat. |
|
V71976 | Forsythoside F (Forsythoside F; Arenarioside) | 94130-58-2 | Forsythoside F is a xanthine oxidase inhibitor that has anti-hyperuric acid effects. |
|
V71974 | Fraxamoside | 326594-34-7 | Fraxamoside is a competitive xanthine oxidase inhibitor (antagonist) with IC50 of 16.1 μM and Ki of 0.9 μM. |
|
V71972 | Ilexoside O | 136552-23-3 | Ilexoside O is a triterpenoid saponin extracted from the roots of Ilex tomentosa. |
|
V70029 | KSK67 | 2566715-93-1 | KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Ki for H3 receptor, sigma-1, and sigma-2 receptors of 3.2, 1531, and 101 nM respectively. |
|
V70045 | KSK68 | 2566715-91-9 | KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7 nM, 3.6 nM, and 22.4 nM for H3 receptors, sigma-1, and sigma-2 receptors, respectively. |
|
V70041 | KSK94 | 2566716-07-0 | KSK94 is a high-affinity histamine H3 receptor antagonist, with Ki for H3 receptor, sigma-1, and sigma-2 receptors of 7.9, 2958, and 75.2 nM respectively. |
|
V70040 | L-693403 maleate | 207455-21-8 | L-693403 maleate is a high-affinity, selective σ ligand. |
|
V71975 | O-Desisobutyl-On-propyl Febuxostat | 1530308-87-2 | O-Desisobutyl-On-propyl Febuxostat information is from patent CN 103467412, which is an inhibitor (blocker/antagonist) of xanthine oxidase. |
|
V70036 | OPC-14523 hydrochloride | 145969-31-9 | OPC-14523 HCl is an orally bioactive sigma and 5-HT1A receptor agonist, targeting sigma receptor (σ1/2 IC50=47/56 nM), 5-HT1A receptor (IC50=2.3 nM) and 5 -HT transporter (IC50=80 nM) has high affinity. |
|
V70035 | Opipramol (Opipramol; Ensidon; G-33040) | 315-72-0 | Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). |
|
V70034 | Panamesine (EMD 57445) | 139225-22-2 | Panamesine (EMD 57445) is a high-affinity sigma receptor ligand with IC50 of 6 nM and may be used in atypical antipsychotic research. |
|
V40083 | PD 144418 oxalate | 1794760-28-3 | PD 144418 oxalate is a novel, high affinity, highly potent and specific sigma 1 (σ1) receptor ligand with Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively. |
|
V71973 | Protosappanin A dimethyl acetal | 868405-37-2 | Protosappanin A dimethyl acetal is a homoisoflavone. |
|
V70032 | Rimcazole dihydrochloride (BW 234U dihydrochloride) | 75859-03-9 | Rimcazole (BW 234U) di-HCl is a carbazole analogue that acts partially as a sigma receptor antagonist. |
|
V70044 | S1R agonist 1 | 193354-70-0 | S1R agonist 1 (Compound 6b) is a selective S1R agonist/activator with Ki of 0.93 nM and 72 nM for S1R and S2R, respectively. |
|
V70042 | S1R agonist 1 hydrochloride | 242487-82-7 | S1R agonist 1 (Compound 6b) HCl is a selective S1R agonist/activator with Ki of 0.93 nM and 2 nM for S1R and S2R, respectively. |
|
V76544 | S1R agonist 2 hydrochloride | S1R agonist 2 (Compound 8b) HCl is a selective S1R agonist/activator with Ki of 1.1 nM and 88 nM for S1R and S2R, respectively. | |
|
V2148 | S1RA (E-52862) | 878141-96-9 | E-52862, also known as S1RA, is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. |
|
V28975 | S1RA (E-52862) HCI | 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). |
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