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Results for "

radioligand binding

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Adrenergic Receptor (11) Amyloid-β (1) Antibiotic (2) Bacterial (2) Cholecystokinin Receptor (1) Cholinesterase (ChE) (2) Cytochrome P450 (1) Drug-Linker Conjugates for ADC (1) Endogenous Metabolite (1) Fluorescent Dye (1) Histamine Receptor (1) iGluR (1) Isotope-Labeled Compounds (6) Lipocalin Family (1) LPL Receptor (3) mAChR (3) Neurokinin Receptor (1) Orexin Receptor (OX Receptor) (1) Serotonin Transporter (1) Sodium Channel (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (8) Endocrinology (1) Infection (3) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (14)

By Targets:

5-HT Receptor (5)

Adrenergic Receptor (11)

Amyloid-β (1)

Antibiotic (2)

Bacterial (2)

Cholecystokinin Receptor (1)

Cholinesterase (ChE) (2)

Cytochrome P450 (1)

Drug-Linker Conjugates for ADC (1)

Endogenous Metabolite (1)

Fluorescent Dye (1)

Histamine Receptor (1)

iGluR (1)

Isotope-Labeled Compounds (6)

Lipocalin Family (1)

LPL Receptor (3)

mAChR (3)

Neurokinin Receptor (1)

Orexin Receptor (OX Receptor) (1)

Serotonin Transporter (1)

Sodium Channel (1)

By Research Areas:

Cancer (1)

Cardiovascular Disease (8)

Endocrinology (1)

Infection (3)

Inflammation/Immunology (2)

Metabolic Disease (3)

Neurological Disease (14)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Emopamil Binding Protein Penicillin-binding protein (PBP) Cdc42-binding kinase ATP-binding cassette (ABC) transporters Oxysterol-binding Protein-related Protein (ORP) FKBP FABP Transthyretin (TTR) Ligands for Target Protein for PROTAC YB-1 SDCBP GHR P-glycoprotein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-141536

PSMA-ALB-56	Drug-Linker Conjugates for ADC	Cancer
PSMA-ALB-56 is a PSMA-targeting radioligand designed by combining the glutamate-urea PSMA-binding entity and an albumin binder .

HY-B1486

Oxprenolol hydrochloride 1 Publications Verification Ba 39089	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-103141

SB-258585 hydrochloride	5-HT Receptor	Neurological Disease
SB-258585 is a high affinity ligand for the 5-HT₆ receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT₆ receptors. SB-258585 can be used to label recombinant and natural 5-HT₆ receptor .

HY-B1486S

Oxprenolol-d7 hydrochloride Ba 39089-d₇	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol-d₇ (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-B1486A

Oxprenolol Ba 39089 free base	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-110223

Atomoxetine-d3 hydrochloride	Adrenergic Receptor	Neurological Disease
Atomoxetine-d3 hydrochloride is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (K_i values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-17385S

Atomoxetine-d5 hydrochloride Tomoxetine-d₅ hydrochloride; LY 139603-d₅; (R)-Tomoxetine-d5 hydrochloride	Isotope-Labeled Compounds Adrenergic Receptor	Neurological Disease
Atomoxetine-d₅ (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-147366

RBP4 ligand-1	Lipocalin Family	Metabolic Disease
RBP4 ligand-1 is a non-retinoid ligands for (RBP4) retinol-binding protein 4. The hRBP4_SPA IC₅₀ and RBP4-TTR FRET IC₅₀ values are 0.23±0.11 and 0.13±0.12 μM in the radioligand binding assay and FRET assay, respectively .

HY-B1486AS

Oxprenolol-d7	Isotope-Labeled Compounds Adrenergic Receptor	Cardiovascular Disease
Oxprenolol-d₇ is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-W008226R

Phloracetophenone (Standard)	Cytochrome P450 Bacterial Antibiotic	Infection Metabolic Disease
Oxprenolol (hydrochloride) (Standard) is the analytical standard of Oxprenolol (hydrochloride). This product is intended for research and analytical applications. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-B1486R

Oxprenolol (hydrochloride) (Standard)	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol (hydrochloride) (Standard) is the analytical standard of Oxprenolol (hydrochloride). This product is intended for research and analytical applications. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-107370AS

(Rac)-Atomoxetine-d7 hydrochloride (Rac)-Tomoxetine d₇ hydrochloride; (Rac)-LY 139603 d₇	Serotonin Transporter Sodium Channel Isotope-Labeled Compounds	Neurological Disease
(Rac)-Atomoxetine-d₇ (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-P1096

A71623	Cholecystokinin Receptor	Metabolic Disease
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC₅₀s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .

HY-118424

JNJ-55511118	iGluR	Neurological Disease
JNJ-55511118 is a highly potent, reversible, and selective AMPA receptor inhibitor selective for TARP-γ8. JNJ-55511118 fully displaces the radioligand (20 nM) with the K_i of 26 nM in competition binding experiments. JNJ-55511118 is a tool molecule with potential therapeutic utility as an anticonvulsant or neuroprotectant .

HY-120792

DAU 5884	mAChR	Others
DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.

HY-133116

4-Hydroxyatomoxetine	Adrenergic Receptor	Neurological Disease
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (K_i values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-122203A

PCS1055 2 Publications Verification	mAChR Cholinesterase (ChE)	Neurological Disease
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC₅₀ of 22 nM and 120 nM for electric eel and human AChE, respectively .

HY-N8295

Leucomycin A13 Kitasamycin A13	Antibiotic	Infection
Leucomycin A13 is a macrolide antibiotic and a component of the leucomycin complex originally isolated from S. kitasatoensis. It is active against B. subtilis, S. aureus, M. luteus, and E. coli with MIC values of 0.16, 0.16, 0.08 and >10 μg/mL, respectively. It binds to ribosomes with an IC₅₀ value of 1.2 μM in a radioligand binding assay.

HY-119005A

YM-49598 iodide	Neurokinin Receptor	Neurological Disease
YM-49598 iodide is a tachykinin NK-1 receptor antagonist. YM-49598 iodide can inhibit drug-induced bladder contraction in rats, with IC₅₀ of 11 μg/kg .

HY-122537

Arotinolol hydrochloride	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites . Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-122537A

Arotinolol	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-10569

Ponesimod 3 Publications Verification ACT-128800	LPL Receptor	Inflammation/Immunology
Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .

HY-167898

MeS-IMPY	Amyloid-β	Neurological Disease
MeS-IMPY is a ligand of β-amyloid plaques. MeS-IMPY shows a high binding affinity to β-amyloid plaques extracted from Alzheimer's disease (AD) human brains or AD brain homogenates compared to IMPY (K_i=7.93 and 8.95 nM, respectively). [ ¹¹C]MeS-IMPY is a potential radioligand for imaging β-amyloid plaques with positron emission tomography (PET) .

HY-103151

CP94253 hydrochloride	5-HT Receptor	Neurological Disease
CP94253 hydrochloride is a potent and selective agonist of 5-HT_1B receptor (K_i= 2 nM in a radioligand binding assay).K_i values for 5-HT_1A, 5-HT_1D, 5-HT_1C and 5-HT₂ receptors are 89, 49, 860, and 1600 nM respectively . CP94253 hydrochloride is centrally active upon systemic administration in vivo .

HY-10569R

Ponesimod (Standard) ACT-128800 (Standard)	LPL Receptor	Inflammation/Immunology
Ponesimod (Standard) is the analytical standard of Ponesimod. This product is intended for research and analytical applications. Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .

HY-W653969

Arotinolol-d5 hydrochloride	Isotope-Labeled Compounds Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-W205529

RO 16-6491 free base	Fluorescent Dye	Neurological Disease
RO 16-6491 Free base is a selective, reversible inhibitor of monoamine oxidase type B (MAO-B), exhibiting high affinity and specificity for binding sites in human frontal cortex mitochondria and platelet membranes. RO 16-6491 demonstrates a fast dissociation of bound radioactivity at 20 degrees C, indicating its dynamic binding properties. RO 16-6491 also acts as a substrate for MAO-B, suggesting that its oxidation may produce a stable intermediate responsible for its potent inhibitory effects. RO 16-6491 serves as an excellent radioligand probe for investigating the regional tissue distribution of MAO-B in various physiological and pathological states.

HY-10569S

Ponesimod-d4 ACT-128800-d₄	Isotope-Labeled Compounds LPL Receptor	Others
Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .

HY-12193

A-349821	Histamine Receptor	Others
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .

HY-122203

PCS1055 dihydrochloride 2 Publications Verification	mAChR Cholinesterase (ChE)	Neurological Disease
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively .

HY-10569S1

Ponesimod-d7 ACT-128800-d₇	Isotope-Labeled Compounds	Others
Ponesimod-d₇ (ACT-128800-d₇) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d₇ (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod-d₇ activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod-d₇ can protect against lymphocyte-mediated tissue inflammation .

HY-103164A

8-(3-Chlorostyryl)caffeine CSC	Endogenous Metabolite	Neurological Disease
8-(3-Chlorostyryl)caffeine (CSC) is an adenosine antagonist with selective activity at the A2a adenosine receptor. 8-(3-Chlorostyryl)caffeine showed 520-fold selectivity in radioligand binding experiments in rat brain. Antagonism of adenylylase by 8-(3-Chlorostyryl)caffeine shows 22-fold selectivity in rat chromaffin cells When 8-(3-Chlorostyryl)caffeine is co-administered with the A1-selective antagonist CPX, It can also further increase exercise activity. 8-(3-Chlorostyryl)caffeine exhibits good MAO-B inhibitory activity in primate mitochondria. 8-(3-Chlorostyryl)caffeine also has excellent A2A receptor affinity .

HY-N8501

Emestrin	Bacterial	Infection
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities. It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC₅₀s=3.94, 0.6, 2.21, 4.55, and 2.21 μg/mL, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC₅₀=5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg/mL) induces apoptosis in HL-60 cells. It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.

HY-10898

SB-674042 1 Publications Verification	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-674042 is a potent and selective non-peptide orexin OX₁ receptor antagonist (K_d=5.03 nM), exhibits 100-fold selectivity for OX₁ over OX₂ receptors with IC₅₀ values of 3.76 nM and 531 nM, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P1096

A71623	Cholecystokinin Receptor	Metabolic Disease
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC₅₀s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W008226R

Phloracetophenone (Standard)	Structural Classification other families Ketones, Aldehydes, Acids Source classification Phenols Polyphenols Plants Curcuma comosa Roxb. Zingiberaceae	Cytochrome P450 Bacterial Antibiotic
Oxprenolol (hydrochloride) (Standard) is the analytical standard of Oxprenolol (hydrochloride). This product is intended for research and analytical applications. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .

Cat. No.	Product Name	Chemical Structure

HY-B1486S

Oxprenolol-d7 hydrochloride
Oxprenolol-d₇ (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-W653969

Arotinolol-d5 hydrochloride
Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

Arotinolol-d5 hydrochloride

Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-10569S1

Ponesimod-d7
Ponesimod-d₇ (ACT-128800-d₇) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d₇ (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod-d₇ activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod-d₇ can protect against lymphocyte-mediated tissue inflammation .

Ponesimod-d7

Ponesimod-d₇ (ACT-128800-d₇) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d₇ (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod-d₇ activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod-d₇ can protect against lymphocyte-mediated tissue inflammation .

HY-17385S

Atomoxetine-d5 hydrochloride
Atomoxetine-d₅ (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-B1486AS

Oxprenolol-d7
Oxprenolol-d₇ is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-107370AS

(Rac)-Atomoxetine-d7 hydrochloride
(Rac)-Atomoxetine-d₇ (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-10569S

Ponesimod-d4
Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .

Ponesimod-d4

Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .

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