260 Results for "

Metabolic stability

" in MedChemExpress (MCE) Product Catalog:
Products (260)

260 Results for "Metabolic stability" in MCE Product Catalog:

4
4 Cited Publications
Cat. No.: HY-P2161B
Target:  

Kisspeptin Receptor

Research Areas:  

Cancer

TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
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3
3 Cited Publications
Cat. No.: HY-16986
CAS No.: 1598383-40-4
Research Areas:  

Cancer

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
3 Cited Publications
Cat. No.: HY-16986A
CAS No.: 1598383-41-5
Research Areas:  

Cancer

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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2
2 Cited Publications
Cat. No.: HY-146302
CAS No.: 2770842-10-7
Purity:  99.00%
Research Areas:  

Cancer

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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2
2 Cited Publications
Cat. No.: HY-156654
CAS No.: 2755812-39-4
Purity:  99.90%
Synonyms: PF-07817883
Target:  

SARS-CoV Virus Protease

Research Areas:  

Infection

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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2
2 Cited Publications
Cat. No.: HY-15163
CAS No.: 1204918-72-8
Synonyms: TG02; SB1317
Target:  

JAK CDK FLT3

Research Areas:  

Cancer

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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1
1 Cited Publications
Cat. No.: HY-107460
CAS No.: 1198408-78-4
Purity:  ≥99.0%
Target:  

Ephrin Receptor

Research Areas:  

Cancer

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
1 Cited Publications
Cat. No.: HY-112388
CAS No.: 626604-39-5
Purity:  99.10%
Target:  

GSK-3

GSK-3b Inhibitor XI (Compound 33) is a potent and selective GSK3β inhibitor, with a Ki value of 25 nM. GSK-3b Inhibitor XI increases glycogen synthase (GS) activity. GSK-3b Inhibitor XI can be used for research on type 2 diabetes and Alzheimer’s disease .
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1
1 Cited Publications
Cat. No.: HY-112613
CAS No.: 1616413-96-7
Purity:  99.59%
Target:  

PI4K

Research Areas:  

Inflammation/Immunology

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
1 Cited Publications
Cat. No.: HY-106225
CAS No.: 355151-12-1
Purity:  99.50%
Synonyms: ZP123
Target:  

Gap Junction Protein

Research Areas:  

Cardiovascular Disease

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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Cat. No.: HY-146486
CAS No.: 2395016-49-4
Purity:  98.09%
Target:  

P2Y Receptor

Research Areas:  

Inflammation/Immunology

P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes .
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Cat. No.: HY-103053
CAS No.: 1529814-60-5
Purity:  96.40%
Target:  

VD/VDR Apoptosis

Research Areas:  

Cancer

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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Cat. No.: HY-163087
CAS No.: 3037561-48-8
Target:  

Orphan GPCR

PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice .
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Cat. No.: HY-144734
CAS No.: 1024168-48-6
Target:  

PANK

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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Cat. No.: HY-144197
CAS No.: 723304-76-5
Purity:  99.50%
Target:  

CCR

Research Areas:  

Neurological Disease

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 .
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Cat. No.: HY-155528
CAS No.: 412008-21-0
Purity:  99.89%
Target:  

Others

Research Areas:  

Others

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 .
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Cat. No.: HY-163032
CAS No.: 3053862-47-5
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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Cat. No.: HY-156280
CAS No.: 3053403-01-0
Purity:  99.07%
Target:  

RAR/RXR

Research Areas:  

Endocrinology

RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC50 of 4.6nM .
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Cat. No.: HY-164793
CAS No.: 733806-89-8
Research Areas:  

Infection

TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis .
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Cat. No.: HY-161993
CAS No.: 3043939-18-7
Target:  

Ketohexokinase

Research Areas:  

Metabolic Disease

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 .
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