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mouse microsomes

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100432
    LOC14
    4 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-150508
    MK-0159
    1 Publications Verification

    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-157421

    NAMPT Metabolic Disease
    Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
    Nampt activator-4
  • HY-40351

    Drug Intermediate Others
    4-Chloro-7H-pyrrolo[2,3-d]pyrimidine is a nitrogen-containing heterocyclic organic synthesis intermediate that can be used for the synthesis of JAK and PKB/Akt inhibitors .
    4-Chloro-7H-pyrrolo[2,3-d]pyrimidine
  • HY-15163
    Zotiraciclib
    2 Publications Verification

    TG02; SB1317

    JAK CDK FLT3 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 .
    Zotiraciclib
  • HY-167856

    GPR88 Neurological Disease
    RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
    RTI-122
  • HY-162455

    EAAT Neurological Disease
    NA-014 is an excitatory amino acid transporter 2 (EAAT2)-selective positive allosteric modulator. NA-014 increases EAAT2-mediated glutamate uptake. NA-014 can be used for the research of epilepsy, neuropathic pain, stroke, drugs of abuse disorders .
    NA-014
  • HY-107460
    LDN-211904 oxalate
    1 Publications Verification

    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

    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-W015782

    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-128268

    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-163032

    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-168328

    NF-κB Interleukin Related Inflammation/Immunology
    FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
    FKK6
  • HY-175533

    Toll-like Receptor (TLR) Neurological Disease Inflammation/Immunology
    TLR2 antagonist-1 is a selective Toll-like receptor 2 (TLR2) antagonist. TLR2 antagonist-1 can effectively inhibit excessive TLR2 activation (IC50 = 11.41 μM) and the production of inflammatory factors. TLR2 antagonist-1 has metabolic stability with a half-life (T1/2) of 16.67 min in mouse liver microsomes. TLR2 antagonist-1 can be used for the researches of inflammation, immunology, and neurological disease .
    TLR2 antagonist-1
  • HY-151229

    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-B1341

    Enidrel; SC-4642; NSC 15432

    Endogenous Metabolite Progesterone Receptor Cancer
    Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
    Norethynodrel
  • HY-143255

    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-118717

    mTOR Cancer
    mTOR inhibitor WYE-28 (compound 28) is a selective inhibitor of mTOR>/b< (IC50)=0.08 nM. mTOR inhibitor WYE-28 inhibits PI3Kα with an IC50 value of 6 nM. mTOR inhibitor WYE-28 shows a metabolic time (T1/2) in nude mouse microsomes of 13 min .
    mTOR inhibitor WYE-28
  • HY-156672

    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-170546

    Haspin Kinase Cancer
    MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes .
    MU1920
  • HY-149920

    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-173235

    Galectin Cardiovascular Disease Inflammation/Immunology Cancer
    Galectin-3-IN-6 (Compound 12) is a human and murine galectin-3 (Gal-3) inhibitor, with an IC50 of 12 nM against human galectin-3, an IC50 of 12.6 nM against mutant murine galectin-3 (V160A), and a Kd of 13 nM for human galectin-3, as well as oral bioavailability. Galectin-3-IN-6 reduces the levels of liver fibrosis markers type I collagen and α-smooth muscle actin in mouse models of acute liver injury and fibrosis. Galectin-3-IN-6 can be used for the research of acute liver injury and fibrosis .
    Galectin-3-IN-6
  • HY-P10331

    SDCBP Cancer
    KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
    KSL 128114
  • HY-153822

    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-136358

    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-146410

    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-117428

    11β-HSD Metabolic Disease
    INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .
    INU-101
  • HY-170491

    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-124084A

    Stearoyl-CoA Desaturase (SCD) Cancer
    SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer .
    SW203668 TFA
  • HY-163291

    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-169194

    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-174150

    Filovirus Infection
    EBOV entry-IN-2 (compound 16) is an EBOV entry inhibitor with an EC50 of 4.42 μM. EBOV entry-IN-2 shows metabolic stability .
    EBOV entry-IN-2
  • HY-169927

    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-N14038

    Fungal Infection
    Crocacin A has anti-yeast and filamentous fungal activity. Crocacin A can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin A can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
    Crocacin A
  • HY-170571

    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-N14040

    Fungal Infection
    Crocacin B has anti-yeast and filamentous fungal activity. Crocacin B can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin B can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
    Crocacin B
  • HY-170486

    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-159088

    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-151578

    Dipeptidyl Peptidase Carbonic Anhydrase Metabolic Disease
    DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively .
    DPP IV/hCA II-IN-1
  • HY-162121

    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-161663

    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-149395

    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-174402

    SARS-CoV Infection
    PLpro-IN-9 (Compound 14e) is a SARS-CoV-2 PLpro inhibitor with an IC50 of 12.0 μM and a KD of 1.86 μM. PLpro-IN-9 has low cytotoxicity but poor metabolic stability. PLpro-IN-9 can be used in the research of SARS-CoV-2 .
    PLpro-IN-9
  • HY-168562

    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-168998

    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-173024

    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-168956

    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-123639

    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-162620

    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
  • HY-159941

    α-synuclein Neurological Disease
    tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
    tau-0N4R-IN-1

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