Search Result
Results for "
affinity labeling
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
65
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-128699
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Dethiobiotin
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Endogenous Metabolite
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Others
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D-Desthiobiotin is a biotin derivative used in affinity chromatography and protein chromatography. D-Desthiobiotin also can be used for protein and cell labeling, detection and isolation .
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- HY-14763S
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RGH-188-d6
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Dopamine Receptor
5-HT Receptor
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Neurological Disease
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Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
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- HY-NP043
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Fluorescent Dye
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Others
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Avidin-Cy3 is Cy3-labeled Avidin. Avidin has excellent affinity with biotin and is often used in combination with biotin for immunoassays to detect the location of antigens in tissues .
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- HY-14763S1
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- HY-107542S
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- HY-D1027
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Monodansyl cadaverine
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Autophagy
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Others
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Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
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- HY-P5830
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Caspase
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Others
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Biotin-DEVD-CHO can be used for affinity labeling of Caspase-8 following in vitro caspase cleavage .
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- HY-D2256
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- HY-107542S2
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- HY-123650
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5'-p-Fluorosulfonylbenzoyladenosine
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Others
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Others
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FSBA? hydrochloride is a useful reagent for the affinity labeling of adenine nucleotide binding proteins and is mainly applied in the study of purified The labeling and subsequent detection of? these proteins can be blocked by including an excess of MgATP, which competes with FSBA for nucleotidebinding sites .
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- HY-14539S
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- HY-14539S2
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- HY-110141
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mGluR
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Others
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ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor .
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- HY-18037
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Phosphodiesterase (PDE)
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Others
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AMG-7980 exhibits high affinity to phosphodiesterase 10A (PDE10A), with a KD of 0.94 nM. AMG-7980 can be used as a tracer of PDE10A, when labeled with radioactive isotope .
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- HY-120842
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mAChR
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Neurological Disease
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RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [ 3H](+)-pentazocine with a Ki of 50 pM .
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- HY-13604S
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Isotope-Labeled Compounds
Androgen Receptor
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Endocrinology
Cancer
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Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
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- HY-P2112
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- HY-149869
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PSMA
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Cancer
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PSMA-IN-3 (compound 17) is a novel high-affinity PSMA inhibitor with an IC50 value of 13 nM. PSMA-IN-3 is suitable for developing an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer .
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- HY-156842
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Amyloid-β
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Neurological Disease
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MCAAD-3 is a near-infrared Aβ imaging probe with blood-brain barrier penetrability. MCAAD-3 has a strong affinity for Aβ polymers (Ki >106 nM) and can label Aβ plaques in the brains of transgenic mice .
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- HY-W001909S
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nAChR
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Metabolic Disease
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Myosmine-d4 is the deuterium labeled Myosmine. Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM[1][2].
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- HY-B0129S
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- HY-18719ES
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Cytochrome P450
Estrogen Receptor/ERR
Drug Metabolite
Parasite
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Cancer
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Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study[1][2].
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- HY-169295
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Biochemical Assay Reagents
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Others
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RAP 1 is a reactive affinity probe (RAP) that selectively labels SLC6A8 in the presence of guanine alanine (GPA). RAP 1 can be used as a chemical probe for identifying and studying potential drug binding sites on SLC6A8 .
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- HY-13619S
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Isotope-Labeled Compounds
Reactive Oxygen Species
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Cancer
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Efaproxiral-d6 is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].
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- HY-157556
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GHSR
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Others
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BPP-2 is a GHSR ligand with an F element. Using 18F isotope labeling BPP-2, a PET probe targeting GHSR can be obtained. The binding affinity Ki of 18F-BPP-2 for GHSR is 274 nM .
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- HY-B0115S
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- HY-12100S
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GSK573719A-d5
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Isotope-Labeled Compounds
mAChR
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Inflammation/Immunology
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Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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- HY-12100S1
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GSK573719A-d10
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mAChR
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Inflammation/Immunology
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Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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- HY-158099
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Celastrol-Biotin
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Biochemical Assay Reagents
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Cancer
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Biotin-Cel (Celastrol-Biotin) is a biotin-labeled Celastrol (HY-13067). Celastrol exhibits antitumor, anti-inflammatory, and anti-obesity activities. Biotin-Cel can be used in biotin-affinity pulldown assay to identify the molecular target of Celastrol in hepatocellular carcinoma cells .
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- HY-B0365AS
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Cytochrome P450
iGluR
Autophagy
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Neurological Disease
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Memantine-d6 (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].
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- HY-13956S
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U 72107-d4
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
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- HY-N6710S
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- HY-B0461S
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mAChR
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Neurological Disease
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
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- HY-B0154S
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- HY-B0154S1
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- HY-B0251S
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Epoxymexrenone-d3
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Mineralocorticoid Receptor
Endogenous Metabolite
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Cardiovascular Disease
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Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
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- HY-119696S
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Isotope-Labeled Compounds
Drug Metabolite
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Neurological Disease
Cancer
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MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
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- HY-B0947S1
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Isotope-Labeled Compounds
Bacterial
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Infection
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Sulfanitran- 13C6 is the 13C labeled Sulfanitran. Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
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- HY-15234S
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Isotope-Labeled Compounds
Glucocorticoid Receptor
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Inflammation/Immunology
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Fluticasone furoate-d3 is deuterium labeled Fluticasone furoate. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment[1][2].
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- HY-15296S1
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- HY-B0652S1
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- HY-B0781S
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Histamine Receptor
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Neurological Disease
Endocrinology
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Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
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- HY-15296S
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- HY-13956S1
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Isotope-Labeled Compounds
PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
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- HY-108411S
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Isotope-Labeled Compounds
Histamine Receptor
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Inflammation/Immunology
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Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
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- HY-103141
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Others
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Neurological Disease
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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 .
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- HY-122607
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Others
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Inflammation/Immunology
Cancer
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DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
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- HY-12987S1
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- HY-B0814S
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(R)-Cetirizine-d4(dihydrochloride)
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Isotope-Labeled Compounds
Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
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- HY-103414S
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Isotope-Labeled Compounds
Dopamine Receptor
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Neurological Disease
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Raclopride-d5 (hydrochloride) is the deuterium labeled Raclopride. Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively[1][2].
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- HY-12987S
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- HY-134308
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Fluorescent Dye
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Others
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8-NBD-cAMP sodium is a fluorescently labeled cyclic adenosine phosphate (cAMP) analogue. 8-NBD-cAMP sodium retains a similar biological activity to cAMP, regulating their activity by binding to specific proteins such as EPACs or PKA. 8-NBD-cAMP sodium can be used in fluorescent competitive binding experiments to evaluate the binding affinity of newly synthesized EPAC1 agonists to EPAC1 proteins .
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- HY-113008AS
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(Z)-Urocanic acid-13C3; cis-UCA-13C3
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Isotope-Labeled Compounds
5-HT Receptor
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Inflammation/Immunology
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cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
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- HY-107322S
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Mepirodipine-d5 hydrochloride; YM-09730-5-d5 hydrochloride
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Isotope-Labeled Compounds
Calcium Channel
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Cardiovascular Disease
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Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
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- HY-12987S2
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- HY-14258AS
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Serotonin Transporter
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Neurological Disease
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Escitalopram-d6 (oxalate) is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
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- HY-14803S
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BMS-214778-d5; VEC-162-d5
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Isotope-Labeled Compounds
Melatonin Receptor
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Neurological Disease
Endocrinology
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Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
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- HY-14258AS1
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(S)-Citalopram-d4 oxalate; (S)-(+)-Citalopram-d4 oxalate
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Isotope-Labeled Compounds
Serotonin Transporter
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Neurological Disease
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Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
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- HY-B0602S2
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Isotope-Labeled Compounds
Serotonin Transporter
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Neurological Disease
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Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
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- HY-B0602S3
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Isotope-Labeled Compounds
Serotonin Transporter
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Neurological Disease
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Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
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- HY-18628S
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Isotope-Labeled Compounds
Bcl-2 Family
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Cancer
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UMI-77-d4 is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
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- HY-13635S
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MK-906-d9
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Isotope-Labeled Compounds
5 alpha Reductase
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Cancer
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Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
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- HY-W008719S
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Mitochondrial Metabolism
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Neurological Disease
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MPP+-d3 (iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT)[1][2].
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- HY-B0814S1
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(R)-Cetirizine-d4
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Isotope-Labeled Compounds
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Inflammation/Immunology
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Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-107322AS1
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Mepirodipine-d5; YM-09730-5-d5 Free base
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Isotope-Labeled Compounds
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Others
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Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
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- HY-123689S
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ALKS-33-d4; RDC-0313-d4
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Isotope-Labeled Compounds
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Neurological Disease
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-A0095S1
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BIMT-17-d4-1; BIMT-17BS-d4-1
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Isotope-Labeled Compounds
5-HT Receptor
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Neurological Disease
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Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
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- HY-B0623AS1
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SKF 101468-d7 hydrochloride
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Dopamine Receptor
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Neurological Disease
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Ropinirole-d7 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
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- HY-B0623AS2
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SKF 101468-d3 hydrochloride
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Dopamine Receptor
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Neurological Disease
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Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
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- HY-B1339AS
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Dicycloverine-d4
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mAChR
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Neurological Disease
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Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
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- HY-B0623AS3
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SKF 101468-d14 hydrochloride
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Dopamine Receptor
Isotope-Labeled Compounds
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Neurological Disease
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Ropinirole-d14 hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
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- HY-D2327
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Dipeptidyl Peptidase
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Others
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DPP-8/9 probe-1 (compound 20) is a fluorescent probe targeting Dipeptidyl Peptidase DPP8/9, which can be selectively labeled and visualized in vitro by fluorescence microscopy Active DPP8/9. DPP-8/9 probe-1 contains a nitrobenzoxadiazole (NBD) tag and has high affinity and selectivity for DPP8/9 over related S9 family members (IC50 of 210 nM and 15 nM, respectively) .
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- HY-B0573BS
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Adrenergic Receptor
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Cardiovascular Disease
Neurological Disease
Endocrinology
|
Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-B0573S
-
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Propranolol-d7 (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-106827S1
-
RU 27987-13C,d3
|
Androgen Receptor
Phosphatase
Progesterone Receptor
Isotope-Labeled Compounds
|
Endocrinology
|
Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
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-
- HY-B0573S1
-
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-16474S
-
TAK-385-d6
|
Isotope-Labeled Compounds
GnRH Receptor
|
Endocrinology
Cancer
|
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
|
-
- HY-D1804
-
|
Fluorescent Dye
|
Others
|
Vari Fluor 680-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=680 nm/701 nm.
|
-
- HY-D1805
-
|
Fluorescent Dye
|
Others
|
Vari Fluor 647-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=650 nm/665 nm.
|
-
- HY-D1806
-
|
Fluorescent Dye
|
Others
|
Vari Fluor 594-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=590 nm/617 nm.
|
-
- HY-D1807
-
|
Fluorescent Dye
|
Others
|
Vari Fluor 555-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=555 nm/565 nm.
|
-
- HY-D1808
-
|
Fluorescent Dye
|
Others
|
Vari Fluor 488-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=490 nm/515 nm.
|
-
- HY-D1809
-
|
Fluorescent Dye
|
Others
|
Vari Fluor 405-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=405 nm/431 nm.
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-
- HY-116450
-
|
Others
|
Neurological Disease
|
TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
|
-
- HY-70057S1
-
FCE 26743-d4-1; EMD 1195686-d4-1
|
Isotope-Labeled Compounds
Monoamine Oxidase
|
Neurological Disease
|
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
|
-
- HY-14541S2
-
LY170053-d8
|
Isotope-Labeled Compounds
Apoptosis
Dopamine Receptor
Autophagy
mAChR
Mitophagy
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-W087187
-
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
|
Cancer
|
DOTAGA-anhydride is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide drug conjugates (RDCs). DOTAGA-anhydride can be used to label monoclonal antibodies (mAbs) such as trastuzumab (targeting HER2/neu receptor with an affinity of 5.5 nM) under mild conditions (PBS pH 7.4, 25 °C, 30 minutes) after chelation with indium-111. [111In-DOTAGA]-trastuzumab showed a tumor uptake of 65% ID/g in mice bearing breast cancer BT-474 xenografts 72 hours after injection, which is valuable for SPECT/CT imaging and biodistribution studies.
|
-
- HY-B0031S3
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].
|
-
- HY-B0031S4
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
|
-
- HY-D1870
-
|
Fluorescent Dye
|
Others
|
Sulfo-Cy3-PEG3-biotin potassium is a biotin-modified derivative of Cy3 (Cyanine3) (HY-D0822) dye containing a TCO group. The TCO group of Sulfo-Cy3-PEG3-biotin potassium reacts with the tetrazine functional group in highly specific click chemistry to form a covalent bond. Thus, Sulfo-Cy3-PEG3-biotin potassium can be covalently bound to some biomolecules (especially antibodies, proteins, etc.) to track their location and dynamic changes in biological samples. And because it is labeled with biotin, it is often used in affinity chromatography experiments, such as immunoprecipitation.
|
-
- HY-B0031S5
-
|
Dopamine Receptor
5-HT Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
- HY-10122S
-
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Endocrinology
Cancer
|
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
|
-
- HY-B1658BS
-
(R)-Frovatriptan-d3 succinate; SB 209509-d3 succinate; VML 251-d3 succinate
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
|
-
Cat. No. |
Product Name |
Type |
-
- HY-D1027
-
Monodansyl cadaverine
|
Fluorescent Dyes/Probes
|
Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
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-
- HY-D1804
-
|
Dyes
|
Vari Fluor 680-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=680 nm/701 nm.
|
-
- HY-D1805
-
|
Dyes
|
Vari Fluor 647-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=650 nm/665 nm.
|
-
- HY-D1806
-
|
Dyes
|
Vari Fluor 594-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=590 nm/617 nm.
|
-
- HY-D1807
-
|
Dyes
|
Vari Fluor 555-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=555 nm/565 nm.
|
-
- HY-D1808
-
|
Dyes
|
Vari Fluor 488-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=490 nm/515 nm.
|
-
- HY-D1809
-
|
Dyes
|
Vari Fluor 405-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=405 nm/431 nm.
|
-
- HY-D2256
-
|
Fluorescent Dyes/Probes
|
BDP TMR ceramide is a BDP TMR (a water-soluble dye with a high affinity to lipid bilayers) labeled ceramide. Ex: 542 nm, Em: 572 nm .
|
-
- HY-D2327
-
|
Fluorescent Dyes/Probes
|
DPP-8/9 probe-1 (compound 20) is a fluorescent probe targeting Dipeptidyl Peptidase DPP8/9, which can be selectively labeled and visualized in vitro by fluorescence microscopy Active DPP8/9. DPP-8/9 probe-1 contains a nitrobenzoxadiazole (NBD) tag and has high affinity and selectivity for DPP8/9 over related S9 family members (IC50 of 210 nM and 15 nM, respectively) .
|
-
- HY-D1870
-
|
Dyes
|
Sulfo-Cy3-PEG3-biotin potassium is a biotin-modified derivative of Cy3 (Cyanine3) (HY-D0822) dye containing a TCO group. The TCO group of Sulfo-Cy3-PEG3-biotin potassium reacts with the tetrazine functional group in highly specific click chemistry to form a covalent bond. Thus, Sulfo-Cy3-PEG3-biotin potassium can be covalently bound to some biomolecules (especially antibodies, proteins, etc.) to track their location and dynamic changes in biological samples. And because it is labeled with biotin, it is often used in affinity chromatography experiments, such as immunoprecipitation.
|
Cat. No. |
Product Name |
Type |
-
- HY-137550
-
|
Enzyme Substrates
|
4-Nitrophenyl β-D-galactopyranoside is a derivative of beta-D-galactoside and monosaccharide. 4-Nitrophenyl β-D-galactopyranoside can be used for affinity label .
|
-
- HY-NP043
-
|
Native Proteins
|
Avidin-Cy3 is Cy3-labeled Avidin. Avidin has excellent affinity with biotin and is often used in combination with biotin for immunoassays to detect the location of antigens in tissues .
|
Cat. No. |
Product Name |
Target |
Research Area |
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14763S
-
|
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
|
-
-
- HY-14763S1
-
|
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
|
-
-
- HY-107542S
-
|
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
|
-
-
- HY-14539S
-
|
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4].
|
-
-
- HY-14539S2
-
|
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4][5].
|
-
-
- HY-W001909S
-
|
Myosmine-d4 is the deuterium labeled Myosmine. Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM[1][2].
|
-
-
- HY-B0129S
-
|
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
|
-
-
- HY-107542S2
-
|
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
|
-
-
- HY-13604S
-
|
Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
|
-
-
- HY-18719ES
-
|
Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study[1][2].
|
-
-
- HY-13619S
-
|
Efaproxiral-d6 is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].
|
-
-
- HY-B0115S
-
|
Pizotyline-d3 is deuterated labeled Pizotifen (HY-B0115). Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
|
-
-
- HY-12100S
-
|
Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
|
-
-
- HY-12100S1
-
|
Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
|
-
-
- HY-B0365AS
-
|
Memantine-d6 (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].
|
-
-
- HY-13956S
-
|
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
|
-
-
- HY-N6710S
-
|
α-Zearalenol-d4 is a deuterated labeled α-Zearalenol . α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER),
α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects .
|
-
-
- HY-B0461S
-
|
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
|
-
-
- HY-B0154S
-
|
Fluticasone propionate-d3 is the deuterium labeled Fluticasone propionate. Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity[1][2].
|
-
-
- HY-B0154S1
-
|
Fluticasone propionate-d5 is deuterium labeled Fluticasone (propionate). Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity[1][2].
|
-
-
- HY-B0251S
-
|
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
|
-
-
- HY-119696S
-
|
MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
|
-
-
- HY-B0947S1
-
|
Sulfanitran- 13C6 is the 13C labeled Sulfanitran. Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
|
-
-
- HY-15234S
-
|
Fluticasone furoate-d3 is deuterium labeled Fluticasone furoate. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment[1][2].
|
-
-
- HY-15296S1
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Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
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- HY-B0652S1
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Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs[1]. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs)[2].
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- HY-B0781S
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Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
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- HY-15296S
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Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
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- HY-13956S1
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Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
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- HY-108411S
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Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
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- HY-12987S1
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Pimozide-d5 N-Oxide is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2].
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- HY-B0814S
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Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
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- HY-103414S
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Raclopride-d5 (hydrochloride) is the deuterium labeled Raclopride. Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively[1][2].
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- HY-12987S
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Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3].
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- HY-113008AS
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cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
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- HY-107322S
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Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
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- HY-12987S2
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Pimozide-d4-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3][4].
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- HY-14258AS
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Escitalopram-d6 (oxalate) is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
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- HY-14803S
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Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
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- HY-14258AS1
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Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
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- HY-B0602S2
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Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
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- HY-B0602S3
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Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
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- HY-18628S
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UMI-77-d4 is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
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- HY-13635S
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Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
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- HY-W008719S
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MPP+-d3 (iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT)[1][2].
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- HY-B0814S1
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Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-107322AS1
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Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
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- HY-123689S
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-A0095S1
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Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
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- HY-B0623AS1
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Ropinirole-d7 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
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- HY-B0623AS2
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Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
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- HY-B1339AS
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Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
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- HY-B0623AS3
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Ropinirole-d14 hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
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- HY-B0573BS
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Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
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- HY-B0573S
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Propranolol-d7 (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
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- HY-106827S1
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Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
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- HY-B0573S1
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Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
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- HY-16474S
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Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
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- HY-70057S1
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Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
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- HY-14541S2
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Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
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- HY-B0031S3
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Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].
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- HY-B0031S4
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Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
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- HY-B0031S5
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Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-10122S
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Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
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- HY-B1658BS
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Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
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- HY-147115
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Azide
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4-Azidophlorizin is a high affinity probe and photoaffinity label for the glucose transporter in brush border membranes . 4-Azidophlorizin is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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