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Mouse liver microsomes

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32

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W015782
    4-Ethylresorcinol

    		Tyrosinase PKA Metabolic Disease Inflammation/Immunology
    4-Ethylresorcinol is a derivative of resorcinol and can serve as a substrate for tyrosinase. 4-Ethylresorcinol has anti-hyperpigmentation and antioxidant effects and can inhibit melanin synthesis. 4-Ethylresorcinol has potential whitening value .
    4-Ethylresorcinol
  • HY-100432
    LOC14
    2 Publications Verification

    		 PDI Neurological Disease Inflammation/Immunology
    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding . LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
    LOC14
  • HY-153822
    JG-23

    		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 .
    JG-23
  • HY-128268
    PFK-IN-1

    		Parasite Infection
    PFK-IN-1 (compound 1) is a phosphofructokinase (PFK) inhibitor, with IC50 values of 0.41 and 0.23 μM against T.brucei and T.cruzi PFK, respectively, and an ED50 of 15.18 μg/mL for T.brucei. The half-lives of PFK-IN-1 in rat and mouse liver microsomes are 9.7 and 408 minutes, respectively .
    PFK-IN-1
  • HY-163291
    AM4085

    		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 .
    AM4085
  • HY-169927
    Ferroptosis-IN-16

    		Ferroptosis Inflammation/Immunology
    Ferroptosis-IN-16 (Compound 13l) is a specific inhibitor for ferroptosis with an EC50 of 0.7 nM and 0.9 nM in ES-2 cell and LX-2 cell. Ferroptosis-IN-16 ameliorates Acetaminophen (HY-66005)-induced acute liver injury in mouse model, and exhibits good metabolic stability in mouse liver microsomes .
    Ferroptosis-IN-16
  • HY-170571
    BE2647

    		Mitochondrial Metabolism Metabolic Disease Inflammation/Immunology
    BE2647 is a selective inhibitor for mitochondrial pyruvate carrier (MPC) with an EC50 of 70 nM. BE2647 exhibits good metabolic stability in mouse liver microsomes. BE2647 can be used in research of metabolic diseases, non-alcoholic fatty liver disease (MASLD), or non-alcoholic steatohepatitis (MASH) .
    BE2647
  • HY-172423
    Darlifarnib

    		Farnesyl Transferase Cancer
    Darlifarnib (Compound (S)-058) is the inhibitor for farnesyl transferase and geranylgeranyltransferase with IC50 ≤ 10 nM and ＞ 1000 nM. Darlifarnib exhibits good metabolic stability in human and mouse liver microsomes with the half-life time ＞ 100 min .
    Darlifarnib
  • HY-169194
    Antimalarial agent 44

    		Parasite Infection
    Antimalarial agent 44 (Compound 3) is an antimalarial agent against parasite. Antimalarial agent 44 has a good permeability across MDCK-MDR1 cell monolayers and a high clearance by mouse liver microsomes .
    Antimalarial agent 44
  • HY-143255
    Enpp-1-IN-11

    		Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
    Enpp-1-IN-11
  • HY-172806
    PARP14 inhibitor 1

    		PARP Inflammation/Immunology
    PARP14 inhibitor 1 (compound Q22) is a selective PARP14 inhibitor with an IC50 of 5.52 nM. PARP14 inhibitor 1 also exhibits anti-inflammatory effects and a half life of 182 min in mouse liver microsomes. PARP14 inhibitor 1 can be utilized in atopic dermatitis research .
    PARP14 inhibitor 1
  • HY-163032
    FABP4-IN-3

    		FABP 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 .
    FABP4-IN-3
  • HY-159088
    KOR agonist 2

    		Opioid Receptor Neurological Disease
    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 .
    KOR agonist 2
  • HY-170486
    MLK3-IN-1

    		Mixed Lineage Kinase FAK Cancer
    MLK3-IN-1 (Compound 37) is a selective inhibitor for mixed-lineage protein kinase 3 (MLK3) with an IC50 <1 nM. MLK3-IN-1 inhibits FAK with an IC50 of 15.5 μM. MLK3-IN-1 exhibits good metabolic stability in mouse and human liver microsomes .
    MLK3-IN-1
  • HY-136358
    LDN-211904

    		Ephrin Receptor Cancer
    LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC .
    LDN-211904
  • HY-149395
    MmpL3-IN-3

    		Bacterial Infection
    MmpL3-IN-3 (Compound 12) is a MmpL3 inhibitor. MmpL3-IN-3 shows a MIC of 0.1 μM against H37Rv. MmpL3-IN-3 shows good stability in mouse liver microsomes. MmpL3-IN-3 can be used for anti-tubercular research .
    MmpL3-IN-3
  • HY-162121
    Antitumor agent-129

    		Others Cancer
    Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC50 value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .
    Antitumor agent-129
  • HY-149920
    Anticancer agent 98

    		Microtubule/Tubulin Cancer
    Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
    Anticancer agent 98
  • HY-161663
    Phosphodiesterase-IN-2

    		Phosphodiesterase (PDE) Cardiovascular Disease
    Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
    Phosphodiesterase-IN-2
  • HY-156672
    S6K2-IN-1

    		FGFR Cancer
    S6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC50: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC50: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes .
    S6K2-IN-1
  • HY-168562
    σ1 Receptor ligand 1

    		Sigma Receptor Neurological Disease Cancer
    σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
    σ1 Receptor ligand 1
  • HY-107460
    LDN-211904 oxalate

    		Ephrin Receptor 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 .
    LDN-211904 oxalate
  • HY-153508
    ANO1-IN-4

    		Chloride Channel Others
    ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
    ANO1-IN-4
  • HY-150508
    MK-0159

    		CD38 Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
    MK-0159
  • HY-151229
    S-Methyl-N,N-diethylthiolcarbamate

    DETC-Me; DDTC-Me; Diethyldithiocarbamic acid methyl ester

    		 Aldehyde Dehydrogenase (ALDH) Metabolic Disease
    S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) is the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram (HY-B0240). It is produced by the methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) inhibits rat liver low Km aldehyde dehydrogenase (ALDH) (ID50=15.5 mg/kg). When administered at a dose of 20.6 mg/kg, it decreases mean arterial pressure (MAP) and increases heart rate in rats during ethanol stimulation.
    S-Methyl-N,N-diethylthiolcarbamate
  • HY-168998
    Yck2-IN-1

    		Fungal Casein Kinase Infection
    Yck2-IN-1 (Compound 2a) is an inhibitor of the fungal Candida albicans Yck2 kinase. It exhibits an IC50 of approximately 80 nM against Yck2 and a MIC80 of 12.5 µM against C. albicans, with good metabolic stability (66% remaining in mouse liver microsomes). In a mouse model of drug-resistant candidiasis, Yck2-IN-1 significantly reduced fungal burden in the kidneys. Yck2-IN-1 holds promise for research in the field of antifungal infection .
    Yck2-IN-1
  • HY-168956
    Pks13-IN-2

    		Bacterial Infection
    Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 shows good metabolic stability in mouse liver microsomes and hepatocytes. Pks13-IN-2 can be used for tuberculosis research .
    Pks13-IN-2
  • HY-146410
    AT2R antagonist 1

    		Angiotensin Receptor Others
    AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
    AT2R antagonist 1
  • HY-123639
    LM-4108

    N-(2-Phenylethyl)-indomethacin amide

    		 COX Inflammation/Immunology Cancer
    LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
    LM-4108
  • HY-173024
    TRPC4/5-IN-3

    		TRP Channel Neurological Disease
    TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
    TRPC4/5-IN-3
  • HY-170491
    GSK-3β inhibitor 23

    		GSK-3 Infection Neurological Disease
    GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
    GSK-3β inhibitor 23
  • HY-162620
    α2A-AR agonist 1

    		Adrenergic Receptor Cancer
    α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
    α2A-AR agonist 1

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