Search Result
Results for "
ICR mouse
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-151563A
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Deubiquitinase
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Cancer
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OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
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- HY-169310
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ATM/ATR
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Cancer
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ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
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- HY-161539
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Opioid Receptor
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Neurological Disease
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KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
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- HY-169919
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Histone Demethylase
Fungal
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Infection
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HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model .
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- HY-169309
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EGFR
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Cancer
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EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure .
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- HY-172113
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PROTACs
YAP
c-Myc
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Cancer
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H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM, and exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki of 2.0, 3.6 and 1.6 nM. H122 downregulates the expression of Myc. H122 inhibits the cell growth of MSTO-211H and NCI-H226 with IC50 of 21.3 nM and 0.6 nM, and exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-151525); Black: linker (HY-W573128); Blue: ligand for E3 ligase Cereblon (HY-W087383))
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- HY-173016
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Opioid Receptor
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Neurological Disease
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HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .
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- HY-162485
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Dengue Virus
Virus Protease
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Infection
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DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
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- HY-19126
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Platelet-activating Factor Receptor (PAFR)
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Infection
Cardiovascular Disease
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CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
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- HY-161523
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Xanthine Oxidase
URAT1
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Metabolic Disease
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XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model .
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- HY-161723
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Dopamine Transporter
CDK
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Neurological Disease
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LH2-051 is a lysosome-enhancing lead compound, which promotes the lysosome biogenesis and the Aβ aggregate clearance through dopamine transporter-cyclin-dependent kinase 9-transcription factor EB (DAT-CDK9-TFEB) pathway. LH2-051 exhibits good pharmacokinetic characteristics in mouse models. LH2-051 is potential for ameliorating Aleheimer’s Disease .
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- HY-120843
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Endothelin Receptor
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Cardiovascular Disease
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WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases .
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- HY-168952
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STING
IFNAR
Interleukin Related
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Inflammation/Immunology
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GHN105 is an orally active inhibitor for STING that inhibits STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. GHN105 reduces the IFN-β, IL-6 and CXCL10 levels in serum, and alleviates colitis in DSS (HY-116282)-induced acute colitis mouse model. GHN105 exhibits good pharmacokinetic parameters in mice with an oral bioavailability of 43% and a half-life of 1.1 hours .
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- HY-159088
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Opioid Receptor
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Neurological Disease
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KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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- HY-170928
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EGFR
Anaplastic lymphoma kinase (ALK)
Cytochrome P450
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Cancer
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DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
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- HY-N1499
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- HY-170448
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PROTACs
Androgen Receptor
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Endocrinology
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PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models . (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))
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- HY-163879
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Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
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Neurological Disease
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hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
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- HY-170450
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- HY-118803
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Factor Xa
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Others
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AS1468240 is an orally active inhibitor for anticoagulant factor Xa (fXa), that inhibits human fXa with IC50 of 8.7 nM. AS1468240 prolongs the coagulation time in mice .
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- HY-164595
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Hippo (MST)
Apoptosis
AMPK
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Metabolic Disease
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IHMT-MST1-39 is an orally active inhibitor for MST kinase, with IC50 of 42 nM and 109 nM, for MST1 and MST2. IHMT-MST1-39 activates the AMPK signaling pathway in liver cells, reduces apoptosis of pancreatic β-cells. IHMT-MST1-39 ameliorates diabetes in Streptozotocin (HY-13753)-induced type 1 diabetes (T1D) mouse models .
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- HY-163923
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Apoptosis
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Cancer
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Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg) .
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- HY-168327
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FXR
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Inflammation/Immunology
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LH10 is a fexaramine-based agonist for FXR with an EC50 of 0.14 μM. LH10 exhibits liver protection efficacy, ameliorates the alpha naphthylisothiocyanate (ANIT)-induced cholestasis, APAP (HY-66005)-induced acute liver injury and non-alcoholic steatohepatitis (NASH) in mouse models .
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- HY-168729
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Bacterial
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Infection
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Antibacterial agent 256 (Compound C09) is an inhibitor for type I signal peptidase (SPase I). Antibacterial agent 256 inhibits gram-positive bacteria, that inhibits S. aureus ATCC 29213, E. faecium QF31, E. faecalis SF23-1 and S. suis P1/7, with MIC of 1-16 μg/mL. Antibacterial agent 256 exhibits cytotoxicity in cancer cell HEp-2 and Caco-2 with CC50 of 14.65 μg/mL and 21.93 μg/mL. Antibacterial agent 256 exhibits a hemolytic activity on mouse RBCs, with an HC50 of 13.29 μg/mL. Antibacterial agent 256 ameliorates the MRSA skin infection in mouse model .
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- HY-161643
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Cholinesterase (ChE)
Keap1-Nrf2
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Neurological Disease
Inflammation/Immunology
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S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
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- HY-153169
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6PPD-Q
1 Publications Verification
6PPD-Quinone
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α-synuclein
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Others
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6PPD-Q (6PPD-Quinone) is an environmental pollutant that can be detected in human urine and is widely present in the environment. 6PPD-Q targets and binds to CNR2, CNR1, AA2AR, LCAT, and TRPA1, with CNR2 exhibiting the highest binding affinity, potentially acting as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q induces intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolysis metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.
6PPD-Q is applicable in research on environmental toxicology, neurodegenerative diseases, and inflammation-related disorders .
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- HY-161627
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NF-κB
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Inflammation/Immunology
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Anemoside A3-methyl 6-aminohexanoate (Compound A3-6) is a derivative of Pulchinenoside C (Anemoside B4) (HY-N0205). Anemoside A3-methyl 6-aminohexanoate inhibits pyruvate carboxylase (PC) with an IC50 of 0.058 μM, reprograms macrophage function, and alleviates DSS-induced colitis through inhibition of the NF-κB and NLRP3 inflammasome pathway. Anemoside A3-methyl 6-aminohexanoate exhibits a moderate in vivo pharmacokinetic characters compared with Anemoside B4 .
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- HY-W436428
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Na+/K+ ATPase
Bacterial
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Infection
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V-161 is the orally active inhibitor for Na +-V-ATPase with an IC50 of 144 nM. V-161 inhibits Enterococcus hirae and Vancomycin-resistant Enterococcus faecium (VRE) under alkaline condition with MIC of 4 µg/mL and 4 µg/mL. V-161 inhibits colonization of VRE in mouse small intestine .
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- HY-P10302A
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GLP Receptor
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Metabolic Disease
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GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-126876
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Apoptosis
AMPK
Reactive Oxygen Species
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Cancer
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GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
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- HY-14849
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Razupenem; SM 216601; SMP 601
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Antibiotic
Bacterial
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Others
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PTZ601 (SMP 601) is an antibiotic, which inhibits the gram-positive bacteria, including the Vancomycin (HY-B0671)-resistant Enterococcus faecium (VREF) and Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). PTZ601 exhibits antimicrobial activity in infected mouse models .
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- HY-168713
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FXR
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Metabolic Disease
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LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
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- HY-148013
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Beta-secretase
NF-κB
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Neurological Disease
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K284-6111 is an orally active inhibitor for protein chitinase 3-like 1 (CHI3L1). K284-6111 reduces the expression of inflammatory proteins such as iNOS, COX-2, GFAP, and Iba-1, inhibits β-secretase and NF-κB, and suppresses Aβ production. K284-6111 ameliorates the Aβ1–42-induced mice memory impairment, and can be used in research about Alzheimer’s Diseases .
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- HY-161893
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Bacterial
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Infection
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Anti-MRSA agent 15 (Compound 9o10) exhibits antibacterial activity, that inhibits methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 0.0625 μg/mL. Anti-MRSA agent 15 exhibits low hemolysis and low cytotoxicity. Anti-MRSA agent 15 exhibits anti-infective in mice .
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- HY-164384
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PI3K
Akt
mTOR
Apoptosis
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Cancer
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DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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- HY-160761
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Opioid Receptor
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Inflammation/Immunology
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K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
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- HY-19606
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Antibiotic MI 43-37F11
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Interleukin Related
NO Synthase
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Metabolic Disease
Inflammation/Immunology
Cancer
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Cytogenin (Antibiotic MI 43-37F11) is an orally active antineoplastic antibiotic. Cytogenin regulates the inflammatory cytokine, reduces the levels of iNOS, NO and IL-6 in mouse macrophages, and exhibits antidiabetic efficacy in mice. Cytogenin inhibits growth of Ehrlich ascites tumor in mouse model .
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- HY-P10435
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Dopamine Receptor
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Neurological Disease
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KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
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- HY-170403
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Histone Demethylase
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Cancer
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LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10302A
-
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GLP Receptor
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Metabolic Disease
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GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-P10435
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Dopamine Receptor
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Neurological Disease
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KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N1499
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- HY-153169
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6PPD-Q
1 Publications Verification
6PPD-Quinone
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Quinones
Structural Classification
Alkaloids
Classification of Application Fields
Other Alkaloids
Source classification
Other Diseases
Benzene Quinones
Endogenous metabolite
Disease Research Fields
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α-synuclein
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6PPD-Q (6PPD-Quinone) is an environmental pollutant that can be detected in human urine and is widely present in the environment. 6PPD-Q targets and binds to CNR2, CNR1, AA2AR, LCAT, and TRPA1, with CNR2 exhibiting the highest binding affinity, potentially acting as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q induces intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolysis metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.
6PPD-Q is applicable in research on environmental toxicology, neurodegenerative diseases, and inflammation-related disorders .
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- HY-120843
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