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Results for "

sigma 1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Sigma Receptor (112) 5-HT Receptor (6) Adrenergic Receptor (1) Akt (3) Amyloid-β (2) Apoptosis (6) ATF6 (2) ATP Synthase (1) Cholinesterase (ChE) (1) Cytochrome P450 (1) Dopamine Receptor (6) Drug Intermediate (1) ERK (1) Ferroptosis (1) GABA Receptor (6) Histamine Receptor (7) iGluR (10) Interleukin Related (1) Isotope-Labeled Compounds (4) mAChR (9) Monoamine Oxidase (2) NF-κB (6) NO Synthase (4) Opioid Receptor (6) Orexin Receptor (OX Receptor) (1) P-glycoprotein (1) Parasite (1) Phospholipase (1) Potassium Channel (2) PPAR (6) Reference Standards (14) SARS-CoV (3) Tau Protein (1) TNF Receptor (1) TRP Channel (3)
By Research Areas:	Cancer (19) Cardiovascular Disease (8) Infection (4) Inflammation/Immunology (16) Metabolic Disease (7) Neurological Disease (102)

By Targets:

Sigma Receptor (112)

5-HT Receptor (6)

Adrenergic Receptor (1)

Akt (3)

Amyloid-β (2)

Apoptosis (6)

ATF6 (2)

ATP Synthase (1)

Cholinesterase (ChE) (1)

Cytochrome P450 (1)

Dopamine Receptor (6)

Drug Intermediate (1)

ERK (1)

Ferroptosis (1)

GABA Receptor (6)

Histamine Receptor (7)

iGluR (10)

Interleukin Related (1)

Isotope-Labeled Compounds (4)

mAChR (9)

Monoamine Oxidase (2)

NF-κB (6)

NO Synthase (4)

Opioid Receptor (6)

Orexin Receptor (OX Receptor) (1)

P-glycoprotein (1)

Parasite (1)

Phospholipase (1)

Potassium Channel (2)

PPAR (6)

Reference Standards (14)

SARS-CoV (3)

Tau Protein (1)

TNF Receptor (1)

TRP Channel (3)

By Research Areas:

Cancer (19)

Cardiovascular Disease (8)

Infection (4)

Inflammation/Immunology (16)

Metabolic Disease (7)

Neurological Disease (102)

120

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Sigma Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101864

Blarcamesine hydrochloride 3 Publications Verification Anavex 2-73	Sigma Receptor	Neurological Disease Cancer
Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC₅₀ of 860 nM.

HY-105296

Blarcamesine 3 Publications Verification	Sigma Receptor mAChR	Cancer
Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .

HY-101484A

NE-100 hydrochloride 1 Publications Verification	Sigma Receptor ATF6	Neurological Disease
NE-100 hydrochloride is an orally active and selective sigma-1 receptor antagonist with an IC₅₀ of 4.16 nM. NE-100 hydrochloride can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE-100 hydrochloride can be used for research on nervous system diseases .

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-125821

Sigma-1 receptor antagonist 1	Sigma Receptor	Neurological Disease
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective **sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (K_i** = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .

HY-18099

S1RA 3 Publications Verification E-52862	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with K_is of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .

HY-18101A

BD-1063 dihydrochloride 3 Publications Verification	Sigma Receptor TRP Channel	Neurological Disease
BD-1063 dihydrochloride is a selective *σ-1* receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

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 and blood-brain barrier permeability 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-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-18099A

S1RA hydrochloride 3 Publications Verification E-52862 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC₅₀ value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .

HY-B2215

Dimemorfan phosphate 3 Publications Verification	Sigma Receptor	Neurological Disease Inflammation/Immunology
Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

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 .

HY-13510

Cutamesine dihydrochloride 5+ Cited Publications 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-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-B1216

Oxeladin citrate	Sigma Receptor	Cardiovascular Disease Others Neurological Disease
Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (K_i = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .

HY-10815

σ1 Receptor antagonist-1 1 Publications Verification	Sigma Receptor Apoptosis	Neurological Disease Cancer
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pK_i=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .

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-125820

Sigma-1 receptor antagonist 3	Sigma Receptor Potassium Channel	Neurological Disease
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a K_i of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC₅₀ of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain .

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-130344

SKF 83959 1 Publications Verification	Dopamine Receptor Sigma Receptor	Neurological Disease
SKF83959 is a potent and selective dopamine D₁-like receptor partial agonist. SKF83959 K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of **sigma (σ)-1** receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression .

HY-14813

Cutamesine 5+ Cited Publications 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-101376

(+)-N-Allylnormetazocine hydrochloride (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride	Opioid Receptor	Neurological Disease
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with K_i values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease .

HY-108512

PD 144418 1 Publications Verification	Sigma Receptor	Neurological Disease
PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (K_i values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity .

HY-P1341

OXA(17-33) Orexin A (17-33) (human, mouse, rat, bovine)	Orexin Receptor (OX Receptor) Sigma Receptor Phospholipase	Neurological Disease
OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC₅₀=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca ²⁺ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy .

HY-100985

IPAG	Sigma Receptor	Cancer
IPAG is a potent sigma-1 receptor antagonist with a pK_i of 4.3 . IPAG induces apoptosis .

HY-101043

4-PPBP maleate	Sigma Receptor iGluR	Neurological Disease
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .

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 selective TMEM97 (a sigma-2 receptor) agonist with a K_i values of 1279 and 46 nM for *σ1R* and σ2R/TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research .

HY-124462

Trifluperidol hydrochloride R 2498	Sigma Receptor	Neurological Disease
Trifluperidol hydrochloride is a Sigma-1 receptor antagonist with a K_i value of 3.3 nM. Trifluperidol hydrochloride is used in the study of psychosis .

HY-116463

E1R	Sigma Receptor	Neurological Disease
E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity .

HY-N15339

Convolamine	Sigma Receptor	Neurological Disease
Convolamine is an alkaloid found in Convolvulus pluricaulis and an effective positive modulator of the *sigma-1* receptor (IC₅₀ = 289 nM), exhibiting cognitive and neuroprotective properties .

HY-B1733

Phenyltoloxamine Bistrimin; Histionex	Histamine Receptor Sigma Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (K_i: 160 nM) .

HY-162759

Sigma-1 receptor antagonist 6	Sigma Receptor	Neurological Disease
Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing *σ1R. Sigma-1* receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015) .

HY-108512A

PD 144418 oxalate 1 Publications Verification	Sigma Receptor	Neurological Disease
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (K_i values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity .

HY-103412

SKF 83959 hydrobromide 1 Publications Verification	Dopamine Receptor Sigma Receptor	Neurological Disease
SKF83959 hydrobromide is a potent and selective dopamine D₁-like receptor partial agonist. SKF83959 hydrobromide K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of **sigma (σ)-1** receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression .

HY-149335

Sigma-1 receptor antagonist 5	Sigma Receptor Histamine Receptor	Neurological Disease
Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH₃R，Ki=7.7 nM，IC₅₀=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models .

HY-116594A

OPC-14523 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
OPC-14523 hydrochloride is an orally active *sigma* and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC₅₀=47/56 nM), the 5-HT1A receptor (IC₅₀=2.3 nM), and the 5-HT transporter (IC₅₀=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .

HY-149274

Sigma-1 receptor antagonist 4	Sigma Receptor	Neurological Disease
Sigma-1 receptor antagonist 4 (Compound 32) is a potent *σ1R* antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance .

HY-116586A

(Rac)-AF710B	mAChR Sigma Receptor	Neurological Disease
(Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .

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-155484

SOMCL-668	Sigma Receptor	Neurological Disease
SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research .

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-131914A

EST64454 hydrochloride	Sigma Receptor	Neurological Disease
EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a K_i of 22 nM. EST64454 hydrochloride has the potential for the research of the pain .

HY-A0172

Captodiame Captodiamine	5-HT Receptor Dopamine Receptor Sigma Receptor	Neurological Disease
Captodiame (Captodiamine) is a 5-HT_2c receptor antagonist and *sigma-1* and D3 dopamine receptor agonist. Captodiame shows antidepressant effect .

HY-153091

BMY 14802	Adrenergic Receptor 5-HT Receptor Sigma Receptor	Neurological Disease
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .

HY-176405

σ1R-IN-1	Sigma Receptor	Neurological Disease
σ1R-IN-1 ((R,R)-1a) is a potent *σ-1R* inhibitor with an IC₅₀ of 110 nM. σ1R-IN-1 is promising for research of neuropsychiatric disorders .

HY-120155

MS-377	Sigma Receptor iGluR	Neurological Disease
MS-377 is a selective and orally active sigma-1 receptor ligand (K_i=73 nM) with weak affinity for sigma-2 receptor (K_i=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (K_i: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia .

HY-168562

σ1 Receptor ligand 1	Sigma Receptor	Neurological Disease Cancer
σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a K_i of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .

HY-147560

σ1 Receptor/μ Opioid receptor modulator 1	Sigma Receptor Opioid Receptor	Neurological Disease
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with K_is of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .

Cat. No.	Product Name	Target	Research Area

HY-P1341

OXA(17-33) Orexin A (17-33) (human, mouse, rat, bovine)	Orexin Receptor (OX Receptor) Sigma Receptor Phospholipase	Neurological Disease
OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC₅₀=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca ²⁺ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113416

Dehydroepiandrosterone sulfate 5 Publications Verification DHEA sulfate; Prasterone sulfate	Human Gut Microbiota Metabolites Microorganisms Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Source Classification	GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-B0765

Dehydroepiandrosterone sulfate sodium 5 Publications Verification DHEA sulfate sodium; Prasterone sulfate sodium	Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Steroids Source Classification	GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-N15339

Convolamine	Alkaloids Convolvulus krauseanus Regel & Schmalh. Quinoline Alkaloids Plants Convolvulaceae Source Classification	Sigma Receptor
Convolamine is an alkaloid found in Convolvulus pluricaulis and an effective positive modulator of the *sigma-1* receptor (IC₅₀ = 289 nM), exhibiting cognitive and neuroprotective properties .

HY-113416R

Dehydroepiandrosterone sulfate (Standard) 1 Publications Verification DHEA sulfate (Standard); Prasterone sulfate (Standard)	Human Gut Microbiota Metabolites Microorganisms Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Source Classification	Reference Standards GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-B0765R

Dehydroepiandrosterone sulfate sodium (Standard) DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)	Structural Classification Endogenous metabolite Steroids Source Classification	Reference Standards GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-N15339A

Convolamine hydrochloride	Structural Classification Alkaloids Microorganisms Tropane Alkaloids Source Classification	Sigma Receptor
Convolamine hydrochloride is a tropane alkaloid and a potent *Sigma-1* receptor positive allosteric modulator with an IC₅₀ value of 289 nM. Convolamine hydrochloride can be extracted from Convolvulus plauricalis. Convolamine hydrochloride exhibits cognitive-improving and neuroprotective properties. Convolamine hydrochloride can be used in research related to Wolfram syndrome and Alzheimer's disease .

Cat. No.	Product Name	Chemical Structure

HY-141921S

Dehydroepiandrosterone sulfate sodium-d6

Dehydroepiandrosterone sulfate sodium salt-d₆ (DHEA sulfate sodium salt-d₆; Prasterone sulfate sodium salt-d₆) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-113416AS

Dehydroepiandrosterone sulfate-d6 sodium dihydrate

Dehydroepiandrosterone sulfate sodium dihydrate-d₆ sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

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 .

HY-18101S

BD-1063-d8 dihydrochloride

BD-1063-d₈ dihydrochloride is the deuterium labeled BD1063 dihydrochloride (HY-18101A) . BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

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