Search Result
Results for "
Metabolic stability
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-146486
-
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P2Y Receptor
|
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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-
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- HY-152479
-
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Topoisomerase
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Cancer
|
Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability .
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-
-
- HY-101930A
-
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11β-HSD
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Metabolic Disease
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(Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of human and mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability .
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-
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- HY-147657
-
|
GABA Receptor
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Neurological Disease
|
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
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-
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- HY-146120
-
|
Bacterial
|
Infection
|
Antitubercular agent-25 (Compound 28) is an anti-tubercular agent with an extracellular IC50 of 0.42 μM and an intracellular IC50 of 0.20 μM against M. tuberculosis H37Rv. Antitubercular agent-25 exhibits good metabolic stability .
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-
-
- HY-103053
-
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VD/VDR
Apoptosis
|
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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-
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- HY-150578
-
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Keap1-Nrf2-IN-12 is a potent Keap1-Nrf2 inhibitor with an IC50 value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes .
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-
-
- HY-149339
-
|
NO Synthase
|
Neurological Disease
|
hnNOS-IN-2 (compound 17) is a human neuronal nitric oxide synthase (hnNOS) inhibitor with good metabolic stability. hnNOS-IN-2 can be used for research in neurodegenerative diseases .
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-
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- HY-107460
-
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Ephrin Receptor
|
Cancer
|
LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC .
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-
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- HY-115981
-
|
HCV Protease
|
Infection
|
NS5A-IN-2 (Compound 33) is a potent inhibitor of NS5A. NS5A-IN-2 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability . NS5A-IN-2 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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-
-
- HY-144286
-
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CXCR
|
Infection
|
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
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-
-
- HY-151340
-
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Bacterial
|
Infection
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Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC50=3.9 μM) .
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-
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- HY-163032
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FABP
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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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-
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- HY-16986
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Histone Methyltransferase
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Cancer
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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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- HY-152473
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Topoisomerase
|
Cancer
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Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism .
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-
-
- HY-16986A
-
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Histone Methyltransferase
|
Cancer
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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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-
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- HY-115982
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|
HCV Protease
|
Infection
|
NS5A-IN-3 (Compound 15) is a potent inhibitor of NS5A. NS5A-IN-3 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability. NS5A-IN-3 exhibits a higher resistance barrier than daclatasvir against genotype 1b . NS5A-IN-3 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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- HY-146617
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Glutaminase
Apoptosis
|
Cancer
|
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
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-
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- HY-145852
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-
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- HY-120438
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PI3K
Akt
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Inflammation/Immunology
|
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research .
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- HY-146616
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Glutaminase
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Cancer
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GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity .
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- HY-150683
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|
Epigenetic Reader Domain
|
Cancer
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NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .
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- HY-150684
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|
Epigenetic Reader Domain
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Cancer
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GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .
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-
-
- HY-163477
-
|
Others
|
Cancer
|
PIP5K1C-IN-2 (compound 33) is a potent and selective 4-phosphate 5-kinases 1 C (PIP5K1C) inhibitor with an IC50 value of 0.0059 µM .
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- HY-150719
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Others
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Cancer
|
AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM .
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-
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- HY-115727
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-
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- HY-155071
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Bacterial
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Infection
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MmpL3-IN-2 is an MmpL3 inhibitor with low cytotoxicity and moderate metabolic stability for tuberculosis research .
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-
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- HY-163087
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-
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- HY-161300
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|
Bacterial
Antibiotic
|
Infection
|
Antibacterial agent 191 (compound 11a) is a potent semi-synthetic antibiotic. Antibacterial agent 191 exhibits preferable metabolic stability .
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-
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- HY-16946
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Acetyl-CoA Carboxylase
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Metabolic Disease
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CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome .
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- HY-148075
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PI4K
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Infection
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PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ, with a mean pIC50 value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum .
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- HY-163291
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Bacterial
|
Infection
|
AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
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-
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- HY-P5984
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mTOR
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Others
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Thioether-cyclized helix B peptide, CHBP can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 .
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- HY-155813
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SARS-CoV
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Infection
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MPI60 is a potent SARS-CoV-2 M Pro inhibitor with high antiviral potency, low cellular cytotoxicity, and high in vitro metabolic stability. MPI60 can be used for SARS-CoV-2 research .
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-
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- HY-15980
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Parasite
|
Infection
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GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
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- HY-149893
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Others
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Metabolic Disease
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MGAT2-IN-4 (compound 33) is an inhibitor of monoacylglycerol transferase 2 (MGAT2), with liver metabolic stability. MGAT2-IN-4 can be used for research on obesity, diabetes and non-alcoholic steatohepatitis (NASH) .
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- HY-135236
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Epigenetic Reader Domain
|
Cancer
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OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity .
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- HY-145872
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HBV
|
Infection
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HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators) .
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-
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- HY-151200
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Steroid Sulfatase
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Endocrinology
|
Steroid sulfatase-IN-4 (Compound 16) is an irreversible steroid sulfatase (STS) inhibitor with an IC50 of 25 nM against human STS. Steroid sulfatase-IN-4 can be used for the research of endometriosis .
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-
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- HY-156280
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RAR/RXR
|
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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-
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- HY-153822
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Tau Protein
|
Neurological Disease
|
JG-23 is a 4-chloro modified analog with ability to promote t-tau degradation. JG-23 exhibits good metabolic stability with a long T1/2 value (36 min) in mouse liver microsome assays .
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- HY-144686
-
|
ATM/ATR
PI3K
mTOR
|
Cancer
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ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability .
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-
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- HY-155528
-
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Others
|
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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-
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- HY-146268
-
|
CaMK
|
Neurological Disease
|
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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-
-
- HY-149242
-
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease .
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-
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- HY-160021
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ROR
|
Inflammation/Immunology
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RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
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-
-
- HY-144653
-
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PDGFR
Apoptosis
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Cancer
|
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma .
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-
-
- HY-156418
-
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DNA/RNA Synthesis
|
Cancer
|
KY386 is a potent, selective inhibitor of DHX33 helicase, with the IC50 of 19 nM. KY386 inhibits U251-MG cells (DHX33-overexpressing cancer cell strain) with IC50 of 20 nM.and shows potent anti-cancer activity and moderate metabolic stability .
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-
-
- HY-112613
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UCB9608
1 Publications Verification
|
PI4K
|
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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-
-
- HY-146121
-
|
Bacterial
|
Infection
|
Antitubercular agent-26 (Compound 32) is an orally active anti-tubercular agent with an extracellular IC50 of 0.50 μM and an intracellular IC50 of 0.51 μM against M. tuberculosis H37Rv. Antitubercular agent-26 shows good metabolic stability, low risk of cardiotoxicity and no genotoxicity .
|
-
- HY-163069
-
|
Bacterial
|
Infection
|
Antitubercular agent-43 (compound A11) is an orally active and potent antitubercular agent. Antitubercular agent-43 shows highly metabolic stability against human and mouse cytochrome P450 enzymes. Antitubercular agent-43 exhibits bactericidal efficacy in acute TB infection mouse model .
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- HY-158316
-
|
Others
|
Others
|
BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumins (HY-W250978)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
|
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- HY-147908
-
|
Adenosine Receptor
|
Inflammation/Immunology
|
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR .
|
-
- HY-147533
-
|
ROR
|
Inflammation/Immunology
|
RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders .
|
-
- HY-126321
-
|
ROR
|
Cancer
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
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- HY-155538
-
|
Others
|
Metabolic Disease
|
Cisd2 agonist 1 (Compound 4q) is a Cisd2 agonist (EC50: 34 nM). Cisd2 agonist 1 enhances the Cisd2 expression and improves the pathological changes in the fatty livers. Cisd2 agonist 1 has good metabolic stability. Cisd2 agonist 1 can be used for research of NAFLD .
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- HY-P5984A
-
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mTOR
|
Others
|
Thioether-cyclized helix B peptide, CHBP (TFA) is the TFA form of Thioether-cyclized helix B peptide, CHBP (HY-P5984). Thioether-cyclized helix B peptide, CHBP (TFA) can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 .
|
-
- HY-160656
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
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-
- HY-147086
-
|
Leukotriene Receptor
G protein-coupled Bile Acid Receptor 1
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases .
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- HY-144687
-
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
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- HY-149470
-
|
Histone Acetyltransferase
|
Cancer
|
MOZ-IN-3 (Compound 6j) is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). MOZ-IN-3 has antitumor activity against four different myeloid leukemia cell lines (HL-60, U937, SKNO-1, K562). MOZ-IN-3 has favorable metabolic stability and pharmacokinetics .
|
-
- HY-106225
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ZP123
|
Gap Junction Protein
|
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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- HY-152468
-
|
Apoptosis
|
Cancer
|
Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
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-
- HY-143330
-
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Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
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- HY-131617
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PGF2α 1,11-lactone
|
Others
|
Others
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Prostaglandin F2α 1,11-lactone is a prostaglandin.
Prostaglandin F2α 1,11-lactone is absorbed by the eye. Prostaglandin F2α 1,
11-Lactone has metabolic stability on the corneal surface and conjunctiva.
Prostaglandin F2α 1,11-lactone can be used in the treatment of glaucoma
.
|
-
- HY-158055
-
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Keap1-Nrf2-IN-20 (Compound ZC9) is an inhibitor for Keap-Nrf2 pathway with KD2 of 51 nM. Keap1-Nrf2-IN-20 exhibits good cell permeability, cell activity, and metabolic stability (serum t1/2 > 24 h) .
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- HY-147758
-
|
Beta-secretase
Amyloid-β
|
Neurological Disease
|
BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability .
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- HY-151964
-
|
Ferroptosis
|
Cancer
|
FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc -), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model .
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- HY-144632
-
|
Fungal
|
Infection
|
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .
|
-
- HY-147754
-
|
Btk
JAK
|
Inflammation/Immunology
|
JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
|
-
- HY-122229
-
|
HIV
|
Infection
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-146594
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM) .
|
-
- HY-146388
-
|
Bacterial
ATP Synthase
|
Infection
|
Mtb ATP synthase-IN-1 (compound 6ab) is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC50 > 64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium .
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- HY-155116
-
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5-HT Receptor
|
Neurological Disease
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5-HT6 agonist 1 (Compound 19) is a 5-HT6 agonist (Ki: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability .
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- HY-100940
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Melatonin Receptor
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Endocrinology
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6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. 6-Chloromelatonin compete for [ 3H]-melatonin and 2-[ 125I]-iodomelatonin binding to MT1 receptors (pKi=8.9 and 9.1, respectively). 6-Chloromelatonin compete for [ 3H]-melatonin binding to MT2 receptors (pKi=9.77) .
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- HY-155746
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JAK
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Infection
Inflammation/Immunology
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JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs) .
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- HY-155992
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Sigma Receptor
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Neurological Disease
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WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
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- HY-157840
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Parasite
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Infection
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Anti-infective agent 9 (compound 1) is a Plasmodium falciparum inhibitor (IC50=600 nM), can downregulate pyruvate levels and TCA cycle in Plasmodium. Anti-infective agent 9It has good metabolic stability and low toxicity to human liver cells. The study found, Anti-infective agent 9Potential targets for inhibiting Plasmodium falciparum are not 1-deoxidation-d-xylulose-5-Phosphate synthase (DXPS) .
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- HY-16750
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GS-9669
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HCV
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Infection
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Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM) .
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- HY-144763
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Apoptosis
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Cancer
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XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research .
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- HY-146302
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Apoptosis
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Cancer
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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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- HY-124623
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Parasite
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Infection
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DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
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- HY-155061
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Cytochrome P450
Aryl Hydrocarbon Receptor
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Cancer
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hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM),as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
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- HY-156102
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Bcr-Abl
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Neurological Disease
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c-ABL-IN-5 is a selective c-Abl inhibitor with neuroprotective effects. c-ABL-IN-5 has blood-brain barrier penetrability, metabolic stability and good pharmacokinetic properties. When c-ABL-IN-5 is labeled with [18F] (compound [18F]3), it can be used as a tracer to evaluate disease-modifying efficacy by complementary positron emission tomography (PET). c-ABL-IN-5 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
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- HY-P2161
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Kisspeptin Receptor
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Cancer
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TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 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 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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- HY-P2161B
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Kisspeptin Receptor
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Cancer
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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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- HY-143880
-
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Mas-related G-protein-coupled Receptor (MRGPR)
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Neurological Disease
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MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
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- HY-P2161A
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Kisspeptin Receptor
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Cancer
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TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA 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 TFA 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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- HY-147319
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Others
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Neurological Disease
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RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
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- HY-155732
-
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Parasite
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Infection
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NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
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- HY-149916
-
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Adenosine Receptor
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Cancer
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A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
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- HY-W250129
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Biochemical Assay Reagents
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Others
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2,3,4,5-Tetrafluorobenzoyl chloride is a fluorinated organic compound that belongs to the class of benzoyl chlorides. It is a colorless liquid with a pungent smell and is mainly used as an intermediate in the synthesis of various pharmaceutical and pesticide compounds. 2,3,4,5-Tetrafluorobenzoyl chloride is an acylating agent that can react with a variety of nucleophiles, including amines, alcohols, and thiols, to form amides, esters, or thioesters, respectively. Its unique fluorine-containing structure can impart desired properties to target molecules, such as increased lipophilicity or increased stability against metabolic degradation. However, due to its high reactivity and potential health hazards, proper safety measures and handling procedures must be followed when using this compound.
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- HY-155050
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Apoptosis
Histone Methyltransferase
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Cancer
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PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
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- HY-156017
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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5-HT6R antagonist 1 (Comopund 8) is a 5-HT6R antagonist (Ki: 5 nM). 5-HT6R antagonist 1 inhibits platelet aggregation. 5-HT6R antagonist 1 has excellent metabolic stability. 5-HT6R antagonist 1 reverses MK-801 (HY-15084B)-induced memory impairments in rats. 5-HT6R antagonist 1 can be used for Alzheimer's disease (AD) research .
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- HY-146201
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Phosphodiesterase (PDE)
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Others
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1 a /5-hydroxynitrile rubber 7 receptor antagonist (5-HT1 a k i = 8 nm, kb= 0.04 nm; 5-nitrile rubber 7K I = 451 nm, kb= 460 nm) has pde4b/pde7a inhibitory activity (PDE4B ic50= 80.4 μ M; Pde7a chip 50= 151.3 μ M)。 Compound 22 has a very good ability of passive penetration of biofilm and high metabolic stability in vitro. In addition, 22's pharmacological evaluation showed its pre cognitive and antidepressant properties in rat behavioral tests.
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HY-L033
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375 compounds
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Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide: e.g. stability against proteolysis (duration of activity) and poor bioavailability. Certain other properties, such as receptor selectivity or potency, often can be substantially improved. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. Hence mimics have great potential in drug discovery.
MCE Peptidomimetic Library contains 375 compounds including peptoid, α-helix mimetics, β-turn/sheets mimetics, etc. This library is an indispensable tool of structure-activity relationships in drug discovery.
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Cat. No. |
Product Name |
Type |
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- HY-W250129
-
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Biochemical Assay Reagents
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2,3,4,5-Tetrafluorobenzoyl chloride is a fluorinated organic compound that belongs to the class of benzoyl chlorides. It is a colorless liquid with a pungent smell and is mainly used as an intermediate in the synthesis of various pharmaceutical and pesticide compounds. 2,3,4,5-Tetrafluorobenzoyl chloride is an acylating agent that can react with a variety of nucleophiles, including amines, alcohols, and thiols, to form amides, esters, or thioesters, respectively. Its unique fluorine-containing structure can impart desired properties to target molecules, such as increased lipophilicity or increased stability against metabolic degradation. However, due to its high reactivity and potential health hazards, proper safety measures and handling procedures must be followed when using this compound.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2161B
-
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Kisspeptin Receptor
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Cancer
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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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- HY-P5984
-
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mTOR
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Others
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Thioether-cyclized helix B peptide, CHBP can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 .
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- HY-P5984A
-
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mTOR
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Others
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Thioether-cyclized helix B peptide, CHBP (TFA) is the TFA form of Thioether-cyclized helix B peptide, CHBP (HY-P5984). Thioether-cyclized helix B peptide, CHBP (TFA) can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 .
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- HY-158055
-
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Keap1-Nrf2
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Inflammation/Immunology
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Keap1-Nrf2-IN-20 (Compound ZC9) is an inhibitor for Keap-Nrf2 pathway with KD2 of 51 nM. Keap1-Nrf2-IN-20 exhibits good cell permeability, cell activity, and metabolic stability (serum t1/2 > 24 h) .
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- HY-P2161
-
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Kisspeptin Receptor
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Cancer
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TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 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 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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- HY-P2161A
-
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Kisspeptin Receptor
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Cancer
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TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA 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 TFA 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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