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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
226 Results for "
Metabolic Stability
" in MedChemExpress (MCE) Product Catalog:
Products (226)
226 Results for "Metabolic Stability" in MCE Product Catalog:
4
4 Cited Publications
Cat. No.: HY-P2161B
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3 Cited Publications
Cat. No.: HY-16986
CAS No.: 1598383-40-4
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EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers . EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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3 Cited Publications
Cat. No.: HY-16986A
CAS No.: 1598383-41-5
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EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers . EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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2 Cited Publications
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14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
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Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .
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Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation .
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1 Cited Publications
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UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent .
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1 Cited Publications
PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer .
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1 Cited Publications
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LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
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1 Cited Publications
Cat. No.: HY-121970
CAS No.: 27031-00-1
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Phosphoglycerate Dehydrogenase (PHGDH) Reactive Oxygen Species (ROS) HIF/HIF Prolyl-Hydroxylase
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iGP-1 is a cell-permeable, selective mixed inhibitor of mitochondrial sn-glycerol-3-phosphate dehydrogenase (mGPDH), with IC50s of 6.3 μM and 13.6 μM for rat mGPDH activity and H2O2 production, respectively. iGP-1 specifically blocks the mitochondrial component of the glycerophosphate shuttle without affecting cytosolic GPDH. iGP-1 not only inhibits cell proliferation and glutaminolysis, and enhances glycolysis, but also significantly alters key cellular physiological processes such as apoptosis, ROS production, HIF-1α stability and mitochondrial membrane potential. iGP-1 remains active in neutrophil cultures under both normoxic and hypoxic conditions, and serves as an ideal probe for glycerol-3-phosphate metabolic mechanisms. iGP-1 has been applied to studies on prostate cancer and related metabolic pathways .
Cat. No.: HY-168046
CAS No.: 2542029-03-6
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ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC50 of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease .
Cat. No.: HY-163087
CAS No.: 3037561-48-8
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PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice .
Cat. No.: HY-144734
CAS No.: 1024168-48-6
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Pantothenate kinase-IN-1 is a PANK3 inhibitor with an IC50 of 0.51 μM. Pantothenate kinase-IN-1 acts as a pantothenate-competitive inhibitor, which occupies the pantothenate-binding site of PANK3 and binds to both protomers in the PANK3 dimer. Pantothenate kinase-IN-1 exhibits metabolic stability in mouse and rat plasma. Pantothenate kinase-IN-1 can be used in the research of pantothenate kinase-associated neurodegenerative diseases and metabolic diseases .
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CCR8 antagonist 1 (Compound 15) is a potente human CCR8 antagonist with a Ki of 1.6 nM. CCR8 antagonist 1 has high safety and metabolic stability. CCR8 antagonist 1 can be used to study diseases such as asthma and multiple sclerosis .
O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability. O4I4 extends lifespan in Caenorhabditis elegans and Drosophila. O4I4 can be used for regenerative medicine and rejuvenation research .
Cat. No.: HY-161993
CAS No.: 3043939-18-7
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BI-9787 is a zwitterionic inhibitior for ketohexokinase, with an IC50 of 12 and 12.8 nM for hKHK-A and hKHK-C. BI-9787 exhibits good metabolic stability in rat hepatocyte and good pharmacokinetic characteristics in rats .
Cat. No.: HY-163032
CAS No.: 3053862-47-5
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology
FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 Ki = 25 ± 3 a nM, FABP3 Ki = 15.03 μM) which exhibits a 601-fold selectivity over FABP3. FABP4-IN-3 also shows metabolic stability and potent cellular anti-inflammatory activity, making it promising to get involved in the research of metabolic disease, cardiac dysfunction and inflammation-related disease .
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CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability .
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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
