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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
44 Results for "
cleft
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "cleft" in MCE Product Catalog:
25
25 Publications Verification
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Endocrinology Cancer
IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
8
Target:
Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis
Research Areas:
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
8
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
4
4 Cited Publications
Cat. No.: HY-B0527AR
CAS No.: 549-18-8
Target:
Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis
Research Areas:
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
3
Research Areas:
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects .
3
Research Areas:
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
Synonyms: NS-2330
Research Areas:
Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent . Tesofensine is a CNS acting anti-obesity agent .
Target:
Environmental Pollutants Apoptosis Insecticide Cholinesterase (ChE) Reactive Oxygen Species (ROS)
Research Areas:
Carbaryl is the inhibitor for acetylcholinesterase that inhibits the degradation of acetylcholine in the synaptic cleft, leads to the accumulation of acetylcholine and causes neurotoxicity. Carbaryl can be used as an insecticide .
Cat. No.: HY-W380450
CAS No.: 46817-91-8
Synonyms: Viloxazin; Emovit
Target:
Research Areas:
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
Synonyms: Viloxazin hydrochloride; Emovit hydrochloride
Target:
Research Areas:
Viloxazine hydrochloride is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50=0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50=32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
Category:
Target:
Cat. No.: HY-W278867
CAS No.: 21956-56-9
Synonyms: trans-Pinosylvin dimethyl ether
Category:
Stilbenes Leguminosae Plants Disease Research Fields Inflammation/Immunology Astragalus membranaceus (Fisch.) Bunge
Target:
trans-3,5-Dimethoxystilbene (trans-Pinosylvin dimethyl ether) is a natural stilbenoid metabolite. trans-3,5-Dimethoxystilbene acts as an acetylcholinesterase inhibitor with a IC50 of 9 μM against Electrophorus electricus acetylcholinesterase. trans-3,5-Dimethoxystilbene binds to acetylcholinesterase and blocks acetylcholine hydrolysis, thereby increasing acetylcholine levels in the cholinergic synaptic cleft. trans-3,5-Dimethoxystilbene can be used in the research of neurodegenerative diseases such as Alzheimer's disease .
Cat. No.: HY-113499B
Target:
Research Areas:
cis-Malonylcarnitine lithium is an ester compound and a metabolite of Malonyl CoA (HY-115899). The level of cis-Malonylcarnitine lithium is closely related to some diseases, such as malonic aciduria, non-syndromic cleft lip with or without cleft palate, etc .
Target:
Reference Standards Insecticide Cholinesterase (ChE) Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
Carbaryl (Standard) is the analytical standard of Carbaryl (HY-B1315). This product is intended for research and analytical applications. Carbaryl is the inhibitor for acetylcholinesterase that inhibits the degradation of acetylcholine in the synaptic cleft, leads to the accumulation of acetylcholine and causes neurotoxicity. Carbaryl can be used as an insecticide.
Cat. No.: HY-B0527AS
CAS No.: 203645-63-0
Cat. No.: HY-B1315S1
CAS No.: 362049-56-7
Cat. No.: HY-14472R
CAS No.: 195875-84-4
Synonyms: NS-2330 (Standard)
Research Areas:
Tesofensine (Standard) is the analytical standard of Tesofensine. This product is intended for research and analytical applications. Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent . Tesofensine is a CNS acting anti-obesity agent .
Target:
Research Areas:
Tetra-N-acetylchitotetraose is a linear chitosan oligosaccharide. Tetra-N-acetylchitotetraose is a component of the hpo-chitoo gosacchaπdes (LCOs) secreted from Rhizobia. Tetra-N-acetylchitotetraose is also a substrate for the Rhizobium leguminosarum nodulation protein NodB, a CO deacetylase .
Cat. No.: HY-W012735
CAS No.: 59045-82-8
Synonyms: (+)-β-Homoproline; (+)-Hexahydronicotinic acid; (+)-3-Carboxypiperidine
Target:
Research Areas:
(+)-Nipecotic acid ((+)-β-Homoproline) is a GABA transport inhibitor with potential antidepressant and anxiolytic activities. (+)-Nipecotic acid can increase the concentration of GABA in the synaptic cleft, thereby enhancing inhibitory neurotransmission. The research on (+)-Nipecotic acid provides a possible direction for the development of new inhibitory compounds for psychiatric diseases .
Cat. No.: HY-16525
CAS No.: 701909-57-1
Research Areas:
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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
