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plasma+stability

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

4

Peptides

1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-41189
    Fmoc-Val-Cit-PAB-PNP

    		ADC Linker Cancer
    Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers .
    Fmoc-Val-Cit-PAB-PNP
  • HY-P10502
    L57

    		LDLR Infection
    L57 is a low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 exhibits high affinity for LRP1, with an EC50 of 45 nM. L57 possesses blood-brain barrier (BBB) permeability and plasma stability. L57 can serve as a carrier for central nervous system drug delivery .
    L57
  • HY-161247
    5-HT2A antagonist 2

    		5-HT Receptor Metabolic Disease
    5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
    5-HT2A antagonist 2
  • HY-P10502A
    L57 acetate

    		LDLR Others
    L57 acetate is a Low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 acetate exhibits high affinity to LRP1 with Ki of 45 nM. L57 acetate exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 acetate can be utilized as the carrier for CNS drug delivery .
    L57 acetate
  • HY-153715
    NV-354

    Mitochondria modulator-1

    		 Biochemical Assay Reagents Metabolic Disease
    NV-354 (Mitochondria modulator-1) (compound 1) is a mitochondrial regulator that stimulates mitochondrial ATP production. NV-354 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. NV-354 has the potential to study mitochondrial diseases .
    NV-354
  • 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-164429
    VIP236

    		Integrin Elastase Cancer
    VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
    VIP236
  • HY-13611
    Diflomotecan

    BN 80915

    		 Topoisomerase Cancer
    Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds .
    Diflomotecan
  • HY-143458
    FAK PROTAC B5

    		FAK PROTACs Cancer
    FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
    FAK PROTAC B5
  • HY-P6053
    KK-103

    		Opioid Receptor Neurological Disease
    KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
    KK-103
  • HY-145842
    Encephalitic alphavirus-IN-1

    		Virus Protease Infection Neurological Disease
    Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC50s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouse plasma stability, and no obvious cytotoxicity .
    Encephalitic alphavirus-IN-1
  • HY-160031
    GLP-1R agonist 19

    		GLP Receptor Cardiovascular Disease
    GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .
    GLP-1R agonist 19
  • HY-155011
    MB076

    		Bacterial Infection
    MB076 is a novel heterocyclic triazole with improved plasma stability. MB076 inhibits seven different Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with Ki values <1 μM. MB076 acts synergistically in combination with multiple cephalosporins to restore pBCSK(-) susceptibility .
    MB076
  • HY-P10973
    Peptide R analogue 10

    		CXCR ERK Cancer
    Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer .
    Peptide R analogue 10
  • HY-175817
    PKMYT1-IN-10

    		Wee1 Apoptosis Cancer
    PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer .
    PKMYT1-IN-10
  • HY-178476
    Anti-MRSA agent 36

    		Bacterial Reactive Oxygen Species (ROS) Infection
    Anti-MRSA agent 36 (Compound III13) is an antibacterial agent with strong anti MRSA activity (MIC = 1 μg/mL). Anti-MRSA agent 36 targets phosphatidylglycerol (PG) on bacterial membranes, disrupting membrane integrity, leading to DNA leakage and increased ROS. Anti-MRSA agent 36 has advantages such as low cytotoxicity, low hemolysis, difficulty in inducing drug resistance, and good plasma stability. Anti-MRSA agent 36 can be used for the study of skin abscess and systemic infection models .
    Anti-MRSA agent 36
  • HY-168118
    Ferroptosis-IN-14

    		Ferroptosis Cancer
    Ferroptosis-IN-14 (compund 36) exhibits the potent anti-ferroptosis activity with an EC50 value of 0.58 ± 0.02 μM and possessed excellent anti-ferroptosis activity, microsomal and plasma stability .
    Ferroptosis-IN-14
  • HY-157998
    mG2N001

    		mGluR Src Others
    mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
    mG2N001
  • HY-156188
    AChE-IN-41

    		Cholinesterase (ChE) Others
    AChE-IN-41 (Compound 2) is a compound of the Galantamine Memantine hybrid. AChE-IN-41 has the inhibition ability of cholinesterase. AChE-IN-41 shows higher plasma stability and comparable microsomal stability in vitro, while showing lower half-life and faster clearance in vivo .
    AChE-IN-41
  • HY-170956
    BTN3A1 ligand-1

    		Drug Intermediate Inflammation/Immunology
    BTN3A1 ligand-1 (Compound 26b) is a triazole-containing aryl/acyloxyalkyl phosphonate prodrug. BTN3A1 ligand-1 can stimulate T cell proliferation (EC50 : 0.49 nM) and interferon γ secretion. BTN3A1 ligand-1 has certain plasma stability and can be used in related immunotherapy research .
    BTN3A1 ligand-1
  • 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-163004
    Type II TRK inhibitor 2

    		Trk Receptor Cancer
    Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
    Type II TRK inhibitor 2
  • 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-161988
    Antimicrobial agent-34

    		Bacterial Infection Inflammation/Immunology
    Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300 .
    Antimicrobial agent-34
  • HY-179390
    KMCA-0011

    		Adrenergic Receptor Neurological Disease
    KMCA-0011 is an orally active ɑ2C adrenoceptor antagonist (Ki = 56.7 nM). KMCA-0011 alleviates depressive behaviors by enhancing BDNF and synaptic plasticity. KMCA-0011 displays favorable metabolic stability, including high plasma stability (99.8% after 120 min). KMCA-0011 can be used for the research of depression .
    KMCA-0011
  • HY-180125A
    Antibacterial agent 307 hydrochloride

    		Bacterial Reactive Oxygen Species (ROS) Infection
    Antibacterial agent 307 hydrochloride is an antibacterial agent. Antibacterial agent 307 hydrochloride shows MICs of 1-4 μg/mL against Gram-positive bacteria, moderate activity against Gram-negative bacteria, low hemolytic toxicity, and excellent plasma stability. Antibacterial agent 307 hydrochloride compromises bacterial membrane integrity via increased permeability and depolarization, induces endogenous ROS accumulation, causes cytoplasmic protein and nucleic acid leakage, and drives rapid bacterial cell death. Antibacterial agent 307 hydrochloride can be used for the research of bacterial infection .
    Antibacterial agent 307 hydrochloride
  • HY-180125
    Antibacterial agent 307

    		Bacterial Reactive Oxygen Species (ROS) Infection
    Antibacterial agent 307 is an antibacterial agent. Antibacterial agent 307 shows MICs of 1-4 μg/mL against Gram-positive bacteria, moderate activity against Gram-negative bacteria, low hemolytic toxicity, and excellent plasma stability. Antibacterial agent 307 compromises bacterial membrane integrity via increased permeability and depolarization, induces endogenous ROS accumulation, causes cytoplasmic protein and nucleic acid leakage, and drives rapid bacterial cell death. Antibacterial agent 307 can be used for the research of bacterial infection .
    Antibacterial agent 307
  • HY-179393
    HBV-IN-54

    		HBV Cancer
    HBV-IN-54 is a selective and orally active HBV inhibitor. HBV-IN-54 exhibits anti-HBV activity in both HepAD38 cells (EC50 = 0.020 μM, CC50 > 100 μM) and HLCZ01 cells (EC50 = 0.024 μM, CC50 > 100 μM). HBV-IN-54 inhibits viral replication in vivo. HBV-IN-54 displays favorable physicochemical properties and high plasma stability. HBV-IN-54 can be used for research on Hepatitis B (HBV) .
    HBV-IN-54
  • 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-159564
    iNOS/COX-2-IN-3

    		COX NO Synthase Inflammation/Immunology
    iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
    iNOS/COX-2-IN-3
  • HY-182042
    DENV-IN-15

    		Dengue Virus Infection
    DENV-IN-15 is a sulfonyl anthranilic acid derivative and a pan-serotype anti-dengue virus (DENV) inhibitor with broad-spectrum anti-RNA virus activity. The EC50 value of DENV-IN-15 against DENV-2 in Huh-7 cells is 0.7 μM. DENV-IN-15 selectively regulates the translation of mRNAs encoding translation-related proteins and containing a 5'-oligopyrimidine tract. DENV-IN-15 reduces the expression of specific ribosomal proteins, thereby inhibiting viral replication. DENV-IN-15 exhibits enhanced membrane permeability, human plasma stability and human liver microsomal metabolic stability. DENV-IN-15 is applicable to research related to dengue virus infection .
    DENV-IN-15
  • HY-181086
    FLT3/HDAC-IN-3

    		FLT3 HDAC Apoptosis Reactive Oxygen Species (ROS) Cancer
    FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3 D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies .
    FLT3/HDAC-IN-3

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