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sigma-2 receptor agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Sigma Receptor (21) Apoptosis (3) Ferroptosis (1) iGluR (1) Interleukin Related (1) Isotope-Labeled Compounds (1) mAChR (4) Opioid Receptor (1) p38 MAPK (1) Potassium Channel (1) Reference Standards (2) SARS-CoV (2) TNF Receptor (1)
By Research Areas:	Cancer (7) Infection (2) Inflammation/Immunology (5) Neurological Disease (14)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Sigma Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

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 .

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 .

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 .

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 .

HY-121033

BS148	Sigma Receptor p38 MAPK Apoptosis	Cancer
BS148 is a selective sigma-2 receptor (S2R) agonist with a K_i 20 nM. BS148 shows >80-fold selective for S2R than S1R. BS148 activates the endoplasmic reticulum stress response through the upregulation of protein kinase R-like ER kinase (PERK), activating transcription factor 4 (ATF4) genes, and C/EBP homologous protein (CHOP). BS148 induces apoptosis in melanoma cell. BS148 downregulates genes related to the cholesterol pathway and activates the MAPK signaling pathway. BS148 can be used for the study of melanoma .

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 .

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-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 .

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 .

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 .

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 .

HY-117731

UKH-1114	Sigma Receptor	Neurological Disease
UKH-1114 is a potent σ2 receptor/Tmem97 agonist with a K_i value of 46 nM, showing antimechanical hypersensitivity effects. UKH-1114 alleviates mechanical hypersensitivity caused by nerve injury without any movement disorders in mice. UKH-1114 is promising for research of neuropathic pain .

HY-178945

KOR agonist 7	Opioid Receptor Interleukin Related TNF Receptor Sigma Receptor	Neurological Disease Inflammation/Immunology
KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a K_i of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .

HY-135608

BD-1008	Sigma Receptor	Neurological Disease
BD-1008 is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor .

HY-100966

BD-1008 dihydrobromide	Sigma Receptor	Neurological Disease
BD-1008 dihydrobromide is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .

HY-134004

Pentoxyverine Carbetapentane	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Carbetapentane) is an orally active **sigma-1 receptor** agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

HY-B1055

Pentoxyverine citrate Carbetapentane citrate	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Carbetapentane) citrate is an orally active **sigma-1 receptor** agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

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 nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .

HY-134004R

Pentoxyverine (Standard) Carbetapentane (Standard)	Reference Standards Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active **sigma-1 receptor** agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

HY-B1055R

Pentoxyverine citrate (Standard) Carbetapentane citrate (Standard)	Reference Standards Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].

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 nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .

BD-1008-d5 dihydrobromide

BD-1008-d₅ dihydrobromide is the deuterium labeled BD-1008 dihydrobromide (HY-100966). BD-1008 dihydrobromide is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .

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