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Results for "

σ2-receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (2) Cholinesterase (ChE) (1) Ferroptosis (1) Histamine Receptor (3) iGluR (1) Monoamine Oxidase (1) Potassium Channel (1) SARS-CoV (2) Sigma Receptor (24)
By Research Areas:	Cancer (9) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (1) Neurological Disease (14)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111669

CT1812 1 Publications Verification Sigma-2 receptor antagonist 1	Sigma Receptor	Neurological Disease
CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant *sigma-2* receptor antagonist with a K_i of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease .

HY-B1813A

(±)-Vesamicol hydrochloride (±)-AH5183 hydrochloride	Sigma Receptor	Neurological Disease
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a K_i of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with K_is of 26 nM and 34 nM, respectively ^[2].

HY-14221A

Siramesine hydrochloride 4 Publications Verification Lu 28-179 hydrochloride	Sigma Receptor Ferroptosis	Cancer
Siramesine (Lu 28-179) hydrochloride is a potent **sigma-2 receptor** agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity ^[2] .

HY-14218

Ditolylguanidine 2 Publications Verification 1,3-Di-o-tolylguanidine; DTG	Sigma Receptor	Neurological Disease
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with K_i values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer ^[2] .

HY-B2087

Glycerol phenylbutyrate HPN-100	Sigma Receptor	Cardiovascular Disease
Glycerol phenylbutyrate is a **sigma-2 (σ2)** receptor ligand, with a pK_i of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent ^[2].

HY-100155

4-IBP	Sigma Receptor	Cancer
4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).

HY-14221

Siramesine Lu 28-179	Sigma Receptor	Cancer
Siramesine (Lu 28-179) is a potent **sigma-2 receptor** agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity ^[2] .

HY-14221B

Siramesine fumarate LU-28-179 fumarate	Sigma Receptor	Cancer
Siramesine (Lu 28-179) fumarate is a potent **sigma-2 receptor** agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity ^[2] .

HY-163075

SYB4	Others	Others
SYB4 (compound 5) is a PET tracer which suitable for imaging the **Sigma-2 Receptor** in the brain of nonhuman primates .

HY-135608

BD-1008	Others	Others
BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.

HY-125819

*Sigma-1 receptor* antagonist 2**	Sigma Receptor	Neurological Disease
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with K_is of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively .

HY-151562

AChE/BuChE/MAO-B-IN-1	Cholinesterase (ChE) Monoamine Oxidase	Neurological Disease
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC₅₀s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ₁ and σ₂ receptors with K_i values of 42.8 nM (human σ₁ receptor) and 191 nM (rat σ₂ receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research .

HY-117420

CM764	Sigma Receptor	Cancer
CM764 is an activator for sigma receptor with K_i of 86.6 and 3.5 nM for sigma-1 receptor and sigma-2 receptor. CM764 increases cytoplasmic calcium, NAD ⁺/NADH, and ATP levels, and decreases the concentration of ROS .

HY-14813

Cutamesine SA4503; AGY 94806	Sigma Receptor	Neurological Disease
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.

HY-B2087R

Glycerol phenylbutyrate (Standard)	Sigma Receptor	Cardiovascular Disease
Glycerol phenylbutyrate (Standard) is the analytical standard of Glycerol phenylbutyrate. This product is intended for research and analytical applications. Glycerol phenylbutyrate is a **sigma-2 (σ2)** receptor ligand, with a pK_i of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent ^[2].

HY-155616

KSK94	Sigma Receptor Histamine Receptor	Neurological Disease
KSK94 is a high-affinity histamine H3 receptor antagonist, with K_is of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .

HY-19469

Roluperidone 1 Publications Verification CYR-101; MIN-101; MT-210	5-HT Receptor Sigma Receptor	Neurological Disease
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for *5-HT_2A* and *sigma-2* receptors (K_i of 7.53 nM and 8.19 nM for 5-HT_2A and sigma-2, respectively).

HY-108513

*σ1 Receptor* antagonist 4**	Sigma Receptor	Neurological Disease
σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a K_i of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (K_i of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .

HY-155615

KSK67	Sigma Receptor Histamine Receptor	Neurological Disease
KSK67 is a high-affinity dual *sigma-2* and histamine H3 receptor antagonist, with K_is of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .

HY-122112

CM572	Sigma Receptor	Cancer
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC₅₀ of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .

HY-107708

threo-Ifenprodil hemitartrate	iGluR Sigma Receptor Potassium Channel	Neurological Disease
threo Ifenprodil hemitartrate is a σ receptor agonist, with K_is of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a *NR2B* subunit-selective NMDA receptor antagonist (IC₅₀=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC ₅₀ of 88 nM, showing antiarrhythmic activity ^[2] .

HY-155614

KSK68	Sigma Receptor Histamine Receptor	Neurological Disease
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with K_is of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .

HY-155992

WLB-89462	Sigma Receptor	Neurological Disease
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (K_i: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .

HY-120421

SW116 free base	Sigma Receptor	Cancer
SW116 free base is a selective fluorescent ligand for **sigma-2 receptor with a K_i** of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research .

HY-145628

CM398	Sigma Receptor	Neurological Disease Inflammation/Immunology
CM398 is a highly selective, orally active **sigma-2 receptor ligand (K_i*=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (K_i=32.90 nM) and serotonin transporters (K_i=244.2* nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .

HY-108511A

PB28	Sigma Receptor Apoptosis SARS-CoV	Infection Cancer
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 is also a σ1 antagonist with a K_i of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate *SARS-CoV-2-human* protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity ^[2] .

HY-108511

PB28 dihydrochloride	Sigma Receptor Apoptosis SARS-CoV	Infection Cancer
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a K_i of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate *SARS-CoV-2-human* protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity ^[2] .

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σ2-receptor

Inhibitors & Agonists