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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
741 Results for "
partial
" in MedChemExpress (MCE) Product Catalog:
Products (741)
741 Results for "partial" in MCE Product Catalog:
Target:
Research Areas:
GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
Cat. No.: HY-187997
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ADAR1-IN-2 is an adenosine analog and an orally active ADAR1 inhibitor with antiproliferative activity against multiple ADAR1-dependent cancer cell lines. ADAR1-IN-2 inhibits ADAR1-mediated A‑to‑I editing of partial RNA substrates (APOBEC3D), thereby activating the RIG‑I/MDA5‑MAVS signaling pathway, inducing G0/G1 cell cycle arrest and apoptosis in tumor cells, and suppressing tumor cell migration and invasion. ADAR1-IN-2 inhibits tumor growth in DU-145 and HUCCT1 xenograft models. ADAR1-IN-2 can be used in research related to cancers such as prostate cancer and breast cancer .
Cat. No.: HY-P1793
CAS No.: 83471-50-5
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Cat. No.: HY-P1793A
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Cat. No.: HY-W027553R
CAS No.: 62732-44-9
Synonyms: NIK-247 free base (Standard); Amiridine free base (Standard)
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Ipidacrine (Standard) is the analytical reference standard of Ipidacrine. This product is used for research and analytical applications. Ipidacrine is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
Cat. No.: HY-W770198
Synonyms: 2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5
Cat. No.: HY-121186R
CAS No.: 42864-78-8
Synonyms: SOM3355 (Standard)
Bevantolol hydrochloride (Standard) (SOM3355 (Standard)) is the analytical standard of Bevantolol hydrochloride (HY-121186). This product is intended for research and analytical applications. Bevantolol hydrochloride (SOM3355) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol hydrochloride blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol hydrochloride reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease .
Cat. No.: HY-121186S
Synonyms: SOM3355-d7
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Bevantolol-d7 hydrochloride (SOM3355-d7) is the d7-labeled Bevantolol hydrochloride (HY-121186). Bevantolol hydrochloride (SOM3355) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol hydrochloride blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol hydrochloride reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease .
Cat. No.: HY-W027553S1
Synonyms: NIK-247-d9 free base
Cat. No.: HY-W680886
CAS No.: 152623-93-3
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6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse .
Cat. No.: HY-177797
CAS No.: 30439-19-1
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5-Methoxytryptoline acts as a modulator of the Serotonin transporter complex, as well as a ligand for the 5-HT2A and 5-HT2C receptors, with Ki values of 130 nM and 140 nM for the 5-HT2A and 5-HT2C receptors, respectively. 5-Methoxytryptoline inhibits the active uptake of Serotonin (HY-B1473A) and Tryptamine (HY-B2132) in platelets. 5-Methoxytryptoline induces behavioral excitation, cortical electroencephalographic desynchronization, and dose-dependent elevation of plasma prolactin, followed by behavioral sedation and partial recovery of cortical electroencephalographic voltage. 5-Methoxytryptoline antagonizes Reserpine (HY-N0480)-induced sedation, reduced locomotor activity, and hypothermia. 5-Methoxytryptoline exerts dose-dependent effects on behavior and cortical electroencephalographic activity in freely moving rats. 5-Methoxytryptoline can be used in depression-related research .
Cat. No.: HY-184086
CAS No.: 139953-73-4
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Cyclazosin is an α1D-adrenergic receptor antagonist and a partial agonist of CXCR4/ACKR3. The pKi values of Cyclazosin for cloned human α1D, α1B and α1A adrenergic receptors are 9.28, 9.23 and 8.18, respectively. Cyclazosin induces β-arrestin recruitment in CXCR4 and ACKR3 with EC50 values of 16 μM and 10 μM, respectively, stimulates ERK1/2 phosphorylation, and induces receptor internalization. Cyclazosin potently inhibits CXCL12-induced chemotaxis of primary human aortic vascular smooth muscle cells. Cyclazosin alters MDMA-induced thermoregulatory responses in mice, converting monophasic hyperthermia to a biphasic pattern without affecting resting core body temperature. Cyclazosin can be used for diseases related to tumor metastasis, MDMA-induced hyperthermia and vasoconstriction .
Cat. No.: HY-N10508
CAS No.: 71204-89-2
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Cat. No.: HY-N10508S
CAS No.: 1637678-42-2
Cat. No.: HY-N0113BR
CAS No.: 6027-23-2
Synonyms: Ordenina hydrochloride (Standard); Peyocactine hydrochloride (Standard)
Category:
Coryphantha vivipara var arizonica Alkaloids Monophenols Cactaceae Other Alkaloids Phenols Plants
Target:
Reference Standards Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Cat. No.: HY-N0113BS
Synonyms: Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride
Target:
Isotope-Labeled Compounds Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
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Hordenine-d6 hydrochloride (Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder .
Cat. No.: HY-N0113A
CAS No.: 62493-39-4
Synonyms: Ordenina sulfate; Peyocactine sulfate
Category:
Target:
Reference Standards Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
