2. Search Result
Search Result
Results for "

pharmacokinetic stability

" in MedChemExpress (MCE) Product Catalog:

47

Inhibitors & Agonists

3

Bibliotecas de Screening

3

Peptides

2

Click Chemistry

Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-160023
    Elisrasib

    D3S-001

    		 Ras PERK Cancer
    Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    Elisrasib
  • HY-112613
    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 .
    UCB9608
  • HY-163763
    T-10418

    		G2A (GPR132) Neurological Disease Inflammation/Immunology Cancer
    T-10418 is a potent and highly selective G2A/GPR132 agonist. T-10418 has an EC50 of 0.82 μM for human G2A activation. T-10418 has good water solubility, metabolic stability, and pharmacokinetic properties. T-10418 can be used for the research of various diseases such as neuropathic pain, acute myeloid leukemia, and inflammation .
    T-10418
  • HY-163099
    P5(PEG24)-VC-PAB-Exatecan

    		Drug-Linker Conjugates for ADC Topoisomerase Apoptosis Cancer
    P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
    P5(PEG24)-VC-PAB-Exatecan
  • HY-149470
    MOZ-IN-3

    		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 .
    MOZ-IN-3
  • HY-161993
    BI-9787

    		Ketohexokinase Metabolic Disease
    BI-9787 is a zwitterionic inhibitior for ketohexokinase, with an IC50 of 12 and 12.8 nM for hKHK-A and hKHK-C. BI-9787 exhibits good metabolic stability in rat hepatocyte and good pharmacokinetic characteristics in rats .
    BI-9787
  • HY-153963
    PF-06655075

    		Oxytocin Receptor Endocrinology
    PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
    PF-06655075
  • HY-144763
    XPO1-IN-1

    		Apoptosis Cancer
    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 .
    XPO1-IN-1
  • HY-121495
    BKI-1369

    		Parasite Infection
    BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
    BKI-1369
  • HY-170546
    MU1920

    		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-159638
    Elunonavir

    		HIV Protease Infection
    Elunonavir (GS-1156) is a HIV protease inhibitor with a high barrier to resistance and excellent metabolic stability. Elunonavir is able to overcome rapid CYP-mediated metabolism, resulting in a significantly prolonged half-life and the potential to reduce dosing frequency without the need for pharmacokinetic enhancers .
    Elunonavir
  • HY-147086
    CAY10789

    		Leukotriene Receptor G protein-coupled Bile Acid Receptor 1 TNF Receptor Metabolic Disease Inflammation/Immunology
    CAY10789 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 .
    CAY10789
  • HY-106095
    DQ 2556

    		Antibiotic Bacterial Penicillin-binding protein (PBP) Infection
    DQ 2556 is a semi-synthetic cephalosporin antibiotic. DQ-2556 exhibits significant activity against both Gram-positive and Gram-negative bacteria, particularly Gram-positive bacteria and Enterobacteriaceae infections. DQ 2556 exerts its bactericidal effect by interfering with cell division. DQ-2556 has a strong affinity for the penicillin-binding proteins (PBPs) of Escherichia coli: PBP1A/1B (IC₅₀ = 0.57-0.73 μg/mL) and PBP3 (IC₅₀ = 0.088 μg/mL). DQ-2556 demonstrates significant in vivo protective effects. DQ-2556 can be used in the development of injectable cephalosporins .
    DQ 2556
  • HY-W043170
    PRL3-CNNM4 PPI-IN-1

    		Phosphatase Cancer
    PRL3-CNNM4 PPI IN 1 (Compound C28d52) is an inhibitor of the PRL3-CNNM4 interaction and also inhibits PRL-mediated suppression of CNNM. PRL3-CNNM4 PPI IN 1 is capable of penetrating epithelial cell layers, exhibits metabolic stability, possesses favorable pharmacokinetic and pharmacodynamic properties, and holds potential for drug development based on this compound .
    PRL3-CNNM4 PPI-IN-1
  • HY-175984
    S1P1 agonist 7

    		LPL Receptor Inflammation/Immunology
    S1P1 agonist 7 is a potent, orally active, and β-arrestin-biased S1P1 agonist (EC50(G‑protein) = 12.7 nM and EC50(β‑arrestin) = 3.23 nM). S1P1 agonist 7 demonstrates potent immunomodulatory activity and a favorable safety profile. S1P1 agonist 7 exhibits excellent metabolic stability, minimal to moderate CYP inhibition, and S1P3-sparing selectivity. S1P1 agonist 7 shows pharmacokinetics, effectively reduces circulating lymphocytes, and significantly alleviates disease severity in experimental autoimmune encephalomyelitis (EAE) mouse models under both prophylactic and therapeutic regimens. S1P1 agonist 7 can be used for multiple sclerosis (MS) research .
    S1P1 agonist 7
  • HY-145713
    GS-8873

    HBV-IN-19

    		 HBV Infection
    GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
    GS-8873
  • HY-158316
    BTL-MK

    		Fc Receptor (FcR) 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 Ovalbumin, low endotoxin (HY-W250978A)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
    BTL-MK
  • HY-120454
    G-479

    		MEK Potassium Channel Cancer
    G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
    G-479
  • HY-153963A
    PF-06655075 TFA

    		Oxytocin Receptor Endocrinology
    PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
    PF-06655075 TFA
  • 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-163797
    WRN inhibitor 10

    		DNA/RNA Synthesis Cancer
    WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
    WRN inhibitor 10
  • HY-131914B
    EST64454 maleate

    		Sigma Receptor Inflammation/Immunology
    EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
    EST64454 maleate
  • HY-122229
    GS-9822

    		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 .
    GS-9822
  • HY-174348
    BRD4-IN-10

    		Epigenetic Reader Domain Inflammation/Immunology
    BRD4-IN-10 (Compound 31) is a selective BRD4 inhibitor with an IC50 of 13.5 nM. BRD4-IN-10 can exert anti-inflammatory and anti-fibrotic effects. BRD4-IN-10 also has good metabolic stability, pharmacokinetic properties and safety. BRD4-IN-10 can be used in the research of renal fibrosis diseases .
    BRD4-IN-10
  • HY-145713A
    GS-8873 TFA

    HBV-IN-19 TFA

    		 HBV Infection
    GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
    GS-8873 TFA
  • HY-159588
    Mcl-1 inhibitor 20

    		Bcl-2 Family Cancer
    Mcl-1 inhibitor 20 (compound 47) is a Mcl-1 inhibitor with anti-leukemic effects. Mcl-1 inhibitor 20 can bind to the BH3 binding groove of Mcl-1 (Ki=24 nM), occupy the P1 pocket in Mcl-1, and form interactions with Lys234 and Val249. Mcl-1 inhibitor 20 has good microsomal stability, pharmacokinetic characteristics and low cardiotoxicity .
    Mcl-1 inhibitor 20
  • HY-161819
    TRK-IN-29

    		Trk Receptor Cancer
    TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
    TRK-IN-29
  • HY-143757
    Cap-dependent endonuclease-IN-10

    		Influenza Virus Infection
    Cap-dependent endonuclease-IN-10 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-10 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo pharmacokinetic and in vivo pharmacodynamic properties, and better hepatic microsomal stability. Cap-dependent endonuclease-IN-10 has the potential for the research of viral infections (including influenza A, influenza B and influenza C) (extracted from patent WO2021129799A1, compound 1-1) .
    Cap-dependent endonuclease-IN-10
  • HY-156102
    c-ABL-IN-5

    		Bcr-Abl Neurological Disease
    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) .
    c-ABL-IN-5
  • HY-159091
    HIV-1 integrase inhibitor 12

    		HIV Integrase Infection
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
    HIV-1 integrase inhibitor 12
  • HY-170887
    MAO-B-IN-39

    		Keap1-Nrf2 Monoamine Oxidase Inflammation/Immunology
    MAO-B-IN-39 (compound11) is a selective monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-39 inhibits MAO-Bwith an IC50 of 3.61 μM. MAO-B-IN-39 demonstrates a potent NRF2 induction capacity. MAO-B-IN-39 exhibits potent anti-inflammatory and neuroprotective activity in OS (oxidative stress)-related in vitro models. MAO-B-IN-39 demonstrates high liver microsomal stability and favorable pharmacokinetics in mice. MAO-B-IN-39 is potential for Parkinson’s disease (PD) research .
    MAO-B-IN-39
  • HY-163799
    PRMT5-MTA-IN-1

    		Histone Methyltransferase Cancer
    PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
    PRMT5-MTA-IN-1
  • HY-164477
    FL442

    		Androgen Receptor Cancer
    FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
    FL442
  • 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-169059
    Ferroptosis-IN-12

    		Ferroptosis Inflammation/Immunology
    Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
    Ferroptosis-IN-12
  • HY-174425
    CYP1B1-IN-9

    		Cytochrome P450 Cancer
    CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance .
    CYP1B1-IN-9
  • HY-180543
    HIV-IN-13 prodrug

    		HIV Infection
    HIV-IN-13 prodrug (Compound 8) is a prodrug of an HIV inhibitor. Without the addition of glutathione (GSH), the HIV-IN-13 prodrug has no antiviral activity, but when 1 mM and 2 mM GSH are added, the EC50 values for HIV-1 are 10 μM and 8.2 μM respectively. HIV-IN-13 prodrug can be used in HIV infection research .
    HIV-IN-13 prodrug
  • HY-180791
    SARS-CoV-2-IN-121

    		SARS-CoV Infection
    SARS-CoV-2-IN-121 (Compound 74) is a SARS-CoV-2 virus inhibitor. SARS-CoV-2-IN-121 exhibits IC50 values in the pseudovirus and live virus systems of 1.6 and 0.45 μM respectively. SARS-CoV-2-IN-121 effectively inhibits the replication or protein expression of the virus within cells and has almost no toxicity to host cells. SARS-CoV-2-IN-121 can be used for SARS-CoV-2 virus infection research .
    SARS-CoV-2-IN-121
  • HY-180919
    ERG-IN-5

    		Potassium Channel Drug Metabolite Cancer
    ERG-IN-5 (Compound M1) is a metabolite of ERG-IN-4 (HY-180918), and it is a hERG potassium channel inhibitor with an IC50 of 1.5 μM. ERG-IN-5 is cytotoxic to MTAP del HCT116 and its CC50 is 28 nM. ERG-IN-5 can be used for the study of colon cancer .
    ERG-IN-5
  • HY-P11416
    Ac-RGDS-NH2

    		Integrin Cardiovascular Disease
    Ac-RGDS-NH2, a tetrapeptide, is an integrin antagonist. Ac-RGDS-NH2 competitively binds to the GPIIb/IIIa receptor (Ki = 4.2 μM), inhibiting the binding of fibrinogen to platelets and thereby effectively suppressing platelet aggregation. Ac-RGDS-NH2 can be used for research on thrombosis .
    Ac-RGDS-NH2
  • HY-174413
    A2AAR antagonist 3

    		Adenosine Receptor Cancer
    A2AAR antagonist 3 is a selective and potent A2A adenosine receptor (A2A AR) antagonist with an IC50 of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A2A AR. A2AAR antagonist 3 demonstrates favorable stability in rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.
    A2AAR antagonist 3
  • HY-181929
    RAI-20

    H018

    		 JAK Inflammation/Immunology
    RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis .
    RAI-20
  • HY-111103A
    CZh226 hydrochloride

    		PAK Cancer
    CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC50 of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma .
    CZh226 hydrochloride
  • HY-165460
    AM-112

    		Antibiotic Beta-lactamase Bacterial Penicillin-binding protein (PBP) Infection
    AM-112 is a β-lactamase (β-lactamase) inhibitor and antibacterial agent, with IC50 values ranging from 0.0002 μg/mL to 0.67 μg/mL against class A, C, and D β-lactamase. By inhibiting PBP2, the penicillin-binding protein of E. coli, and protecting Ceftazidime (HY-B0593) from enzymatic hydrolysis, AM-112 significantly enhances the antibacterial efficacy of Ceftazidime against Gram-negative bacteria, enterococci, and staphylococci. AM-112 exhibits favorable pharmacokinetic properties and acid-base stability. AM-112 can be used for the research of bacterial infections .
    AM-112
  • HY-W663179
    DNDI-VL-2098

    		Parasite Cytochrome P450 Infection
    DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .
    DNDI-VL-2098
  • HY-182355
    MTHFD2-IN-7

    		Methylenetetrahydrofolate Dehydrogenase (MTHFD) Cancer
    MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
    MTHFD2-IN-7
  • HY-180525
    PB2-IN-2

    		Influenza Virus Infection
    PB2-IN-2 is an orally active PB2 inhibitor with RNA-dependent RNA Polymerase (RNP) IC50 = 0.2 nM, LRA (Ligand Receptor Assay) EC50 = 0.8 nM, Cytopathic Effect (CPE) EC50 = 0.1 nM. PB2-IN-2 exhibits broad-spectrum, nanomolar antiviral potency against a panel of influenza A strains (including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, rPR8(H1N1)/H7N9 with EC50 = 1.5, 3.6, 3.7, 13.8, 2.9 and 9.8 nM and all the CC50 values > 2 μM. PB2-IN-2 possesses an excellent pharmacokinetic profile and metabolic stability. PB2-IN-2 can be used for anti-influenza research .
    PB2-IN-2

Consulta en línea

Your information is safe with us. * Required Fields.

Saludo

  

Country or Region *

Nombre del solicitante *

 

Nombre de la Organizaciòn *

Department *

     

Direcciòn del E-mail *

 

Nombre del producto *

Cat. No.

  

Requested quantity *

Número de teléfono *

     

Observaciones

Consulta en línea

Inquiry Information

Nombre del producto:
Cat. No.:
Cantidad:
MCE Japan Authorized Agent: