Search Result

Results for "

σ2-receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Adrenergic Receptor (1) Apoptosis (2) Cholinesterase (ChE) (1) Dopamine Receptor (1) Ferroptosis (1) Histamine Receptor (4) iGluR (1) Isotope-Labeled Compounds (1) mAChR (1) Monoamine Oxidase (1) Potassium Channel (1) Reference Standards (1) SARS-CoV (2) Sigma Receptor (33)
By Research Areas:	Cancer (9) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (1) Neurological Disease (22)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111669

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

HY-B1813A

(±)-Vesamicol hydrochloride 1 Publications Verification (±)-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-14221

Siramesine 5 Publications Verification 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-14221A

Siramesine hydrochloride 5 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-174155

Sigma-2 Receptor ligand 1	Sigma Receptor	Neurological Disease
Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective **Sigma-2 receptor ligand with a K_i** value of 40 nM. Sigma-2 Receptor ligand 1 is promising for research of Alzheimer's disease .

HY-14222

UMB24	Sigma Receptor	Neurological Disease
UMB24 is a potent antagonist of σ2 receptor, with K_i values of 170 nM anf 322 nM for σ2 receptor and σ1 receptor, respectively. UMB24 attenuats cocaine-induced convulsions and locomotor activity, but not lethality .

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

HY-14218R

Ditolylguanidine (Standard)	Sigma Receptor	Neurological Disease
Ditolylguanidine (Standard) is the analytical standard of Ditolylguanidine. This product is intended for research and analytical applications. Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki 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 1 Publications Verification 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-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-14813

Cutamesine Maximum Cited Publications 6 Publications Verification SA4503; AGY 94806	Sigma Receptor	Neurological Disease
Cutamesine (SA4503) is a potent and selective sigma 1 receptor agonist with an IC₅₀ of 17.4 nM in guinea pig brain membranes. Cutamesine shows >100-fold less affinity for the sigma 2 receptor (IC₅₀ of 1784 nM). Cutamesine has antidepressant effects ^[2].

HY-13510

Cutamesine dihydrochloride Maximum Cited Publications 6 Publications Verification SA4503 dihydrochloride; AGY94806 dihydrochloride	Sigma Receptor	Neurological Disease
Cutamesine (SA4503) dihydrochloride is a potent and selective sigma 1 receptor agonist with an IC₅₀ of 17.4 nM in guinea pig brain membranes. Cutamesine dihydrochloride shows >100-fold less affinity for the sigma 2 receptor (IC₅₀ of 1784 nM). Cutamesine dihydrochloride has antidepressant effects ^[2].

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-B2087R

Glycerol phenylbutyrate (Standard) HPN-100 (Standard)	Reference Standards 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-135608

BD-1008	Sigma Receptor	Neurological Disease
BD-1008 is a selective sigma 1 (σ1) receptor antagonist with a K_i of 2 nM. BD-1008 exhibits 4-fold selectivity over the sigma-2 receptor (K_i of 8 nM). BD-1008 can be used for the study of neurological diseases ^[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-169185

Sigma-2 Radioligand 2	Sigma Receptor	Cancer
Sigma-2 Radioligand 2 (compund 4) exhibits low nanomolar affinity (Ki(σ2)=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor .

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-100966

BD-1008 dihydrobromide	Sigma Receptor	Neurological Disease
BD-1008 dihydrobromide is a selective sigma 1 (σ1) receptor antagonist with a K_i of 2 nM. BD-1008 dihydrobromide exhibits 4-fold selectivity over the sigma-2 receptor (K_i of 8 nM). BD-1008 dihydrobromide can be used for the study of neurological diseases ^[2].

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-100966S

BD-1008-d5 dihydrobromide	Isotope-Labeled Compounds Sigma Receptor	Neurological Disease
BD-1008-d₅ dihydrobromide is the deuterium labeled BD-1008 dihydrobromide (HY-100966) . BD-1008 dihydrobromide is a selective sigma 1 (σ1) receptor antagonist with a K_i of 2 nM. BD-1008 dihydrobromide exhibits 4-fold selectivity over the sigma-2 receptor (K_i of 8 nM). BD-1008 dihydrobromide can be used for the study of neurological diseases ^[2] .

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] .

HY-172339

4-AcO-DALT hydrochloride 4-Acetoxy DALT hydrochloride	5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor mAChR Sigma Receptor	Neurological Disease
4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, *histamine receptor* 1 (H1)*, muscarinic M2 receptor* and **Sigma 2 receptor. 4-AcO-DALT hydrochloride shows K_i** values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors ^[2].

Cat. No.	Product Name	Chemical Structure

HY-100966S

BD-1008-d5 dihydrobromide
BD-1008-d₅ dihydrobromide is the deuterium labeled BD-1008 dihydrobromide (HY-100966) . BD-1008 dihydrobromide is a selective sigma 1 (σ1) receptor antagonist with a K_i of 2 nM. BD-1008 dihydrobromide exhibits 4-fold selectivity over the sigma-2 receptor (K_i of 8 nM). BD-1008 dihydrobromide can be used for the study of neurological diseases ^[2] .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: