Sigma Receptor

Sigma Receptor

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.

Sigma Receptor related products

Structure Cat No. Product Name CAS No. Product Description
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).
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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