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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
872 Results for "
Noncompetitive modulation
" in MedChemExpress (MCE) Product Catalog:
Products (872)
872 Results for "Noncompetitive modulation" in MCE Product Catalog:
12
12 Cited Publications
Synonyms: NP-120; RC-61-91
Research Areas:
Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
12
12 Cited Publications
Synonyms: NP-120 tartrate; RC-61-91 tartrate
11
11 Cited Publications
Synonyms: Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
Category:
Flavonoids Glycine max (L.) merr Metabolic Disease Phenols Polyphenols Leguminosae Extract Plants Disease Research Fields Isoflavones
Target:
11
Target:
Research Areas:
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects .
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11 Cited Publications
Synonyms: 6-Methoxynicotinamide
Target:
Research Areas:
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
11
Target:
Research Areas:
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma .
11
11 Cited Publications
Synonyms: SP-2577 mesylate
Target:
Research Areas:
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma .
10
10 Cited Publications
Synonyms: AS703026; MSC1936369B
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
10
10 Cited Publications
Target:
Research Areas:
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
10
10 Cited Publications
Target:
Research Areas:
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects . MPEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
9
9 Cited Publications
Cat. No.: HY-W107464
CAS No.: 2457232-14-1
Target:
Research Areas:
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells .
8
8 Cited Publications
Cat. No.: HY-17353
CAS No.: 321674-73-1
Target:
Research Areas:
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
8
8 Cited Publications
Synonyms: Trodusquemine lactate; Aminosterol-1436 lactate
Target:
Research Areas:
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
8
Target:
Research Areas:
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
8
8 Cited Publications
Cat. No.: HY-19870
CAS No.: 920014-72-8
Synonyms: RM-493; BIM-22493; IRC-022493
Target:
Setmelanotide (RM-493) is a blood-brain barrier-permeable, selective MC4R agonist with a Ki value of 2.1 nM for hMC4R. Setmelanotide activates the CaMKK2/AMPK signaling pathway. Setmelanotide mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression .
8
8 Cited Publications
Cat. No.: HY-19870C
CAS No.: 2759937-80-7
Synonyms: RM-493 monoacetate; BIM-22493 monoacetate; IRC-022493 monoacetate
Target:
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
7
Research Areas:
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
7
Filanesib hydrochloride (ARRY-520 hydrochloride) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib hydrochloride induces cell death by apoptosis in vitro. Filanesib hydrochloride has potent anti-proliferative activity .
7
7 Cited Publications
Target:
Research Areas:
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
7
Target:
Research Areas:
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
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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
