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plasma stability

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57

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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-107749
    ML 190

    		Opioid Receptor Neurological Disease
    ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively .
    ML 190
  • HY-150719
    AIMP2-DX2-IN-1

    		Aminoacyl-tRNA Synthetase Cancer
    AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM .
    AIMP2-DX2-IN-1
  • 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-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-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-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-150681
    SARS-CoV-2 nsp14-IN-2

    		SARS-CoV Infection
    SARS-CoV-2 nsp14-IN-2 is a potent SARS-CoV-2 Nsp14 methyltransferase inhibitor with an IC50 value of 0.093 µM. SARS-CoV-2 nsp14-IN-2 shows antiviral activity. SARS-CoV-2 nsp14-IN-2 shows plasma and liver S9 stability. SARS-CoV-2 nsp14-IN-2 has the potential for the research of COVID-19 .
    SARS-CoV-2 nsp14-IN-2
  • 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-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-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-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-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-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-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-155047
    BDM91514

    		Bacterial Infection
    BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability .
    BDM91514
  • HY-172093
    HIV-1 inhibitor-80

    		HIV Infection
    HIV-1 inhibitor-80 (compound M44) is an HIV-1 inhibitor with an EC50 of 5-148 nM. HIV-1 inhibitor-80 shows good metabolic stability and cytotoxicity in human plasma and human liver microsomes .
    HIV-1 inhibitor-80
  • 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-P10502
    L57

    		LDLR Others
    L57 exhibits high affinity to the low-density lipoprotein receptor-related protein 1 (LRP1) with Ki of 45 nM. L57 exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 can be utilized as the carrier for CNS drug delivery .
    L57
  • HY-126254
    BI-4924
    1 Publications Verification

    		 Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
    BI-4924
  • HY-153715
    NV-354

    Mitochondria modulator-1

    		 Biochemical Assay Reagents Metabolic Disease
    Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases .
    NV-354
  • HY-155011
    MB076

    		Bacterial Antibiotic Others
    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-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-118147
    ML356

    		Fatty Acid Synthase (FASN) Cancer
    ML356 (Compound 16) is an inhibitor for fatty acid synthase (FAS), that inhibits the thioesterase domain of FAS (FAS TE) with an IC50 of 0.334 μM, and blocks the de novo palmitate synthesis in PC-3 cell with an IC50 of 20 μM. ML356 exhibits good membrane permeability, and good stability in human and mouse plasma .
    ML356
  • HY-117187
    Corr4A

    		CFTR Others
    Corr4A is a chemical corrector, which can be used for cystic fibrosis. Corr4A interacts directly with the cystic fibrosis transmembrane conductance regulator (CFTR) or affects indirectly its folding process. Corr4A increases the expression of CFTR ΔF508 on the cell surface, thereby improving its transport to the plasma membrane and increasing the stability of the rescued mutant protein .
    Corr4A
  • HY-147547
    SV5

    		Amyloid-β Neurological Disease
    SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against Aβ1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile .
    SV5
  • 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-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-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-163403
    VEGFR-2-IN-43

    		VEGFR Cardiovascular Disease Cancer
    VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
    VEGFR-2-IN-43
  • HY-144771
    SARS-CoV-2-IN-14

    		SARS-CoV Infection
    SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
    SARS-CoV-2-IN-14
  • HY-144772
    SARS-CoV-2-IN-15

    		SARS-CoV Infection
    SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
    SARS-CoV-2-IN-15
  • HY-144770
    SARS-CoV-2-IN-13

    		SARS-CoV Infection
    SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
    SARS-CoV-2-IN-13
  • HY-143877
    NN-390

    		HDAC Cancer
    NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
    NN-390
  • HY-128943
    MAC glucuronide phenol-linked SN-38

    		Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
    MAC glucuronide phenol-linked SN-38
  • HY-170509
    Ferroptosis-IN-17

    		Ferroptosis Glutathione Peroxidase Cardiovascular Disease Neurological Disease Cancer
    Ferroptosis-IN-17 (Compound 18) is a ferroptosis (Ferroptosis) inhibitor with an EC50 value of 0.57 μM. Ferroptosis-IN-17 reduces intracellular ferrous ion accumulation, lipid peroxidation, and effectively restores the levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). Ferroptosis-IN-17 shows good solubility and significant metabolic stability in rat plasma. Ferroptosis-IN-17 is promising for research in tumor suppression, neurodegenerative diseases, and cardiovascular diseases .
    Ferroptosis-IN-17
  • HY-172090
    MASP-2-IN-1

    		Ser/Thr Protease Potassium Channel Inflammation/Immunology
    MASP-2-IN-1 (Compound 77) is the inhibitor for mannan-binding lectin-associated serine protease (MASP), that inhibits MASP2 and MASP3 with IC50 of 11.4 nM and 13.2 µM. MASP-2-IN-1 exhibits a weak inhibitory activity against hERG with an IC50 of 175 µM. MASP-2-IN-1 reveals a poor stability in mouse plasma with a half-life of 4.4 hours .
    MASP-2-IN-1
  • HY-158082
    TRITC-dextran, MW 4000
    1 Publications Verification

    Tetramethyl rhodamine isothiocyanate glucan, MW 4000

    		 Fluorescent Dye Others
    TRITC-dextran MW 4000 (Tetramethyl rhodamine isothiocyanate glucan, MW 4000) is a fluorescent dye, with the molecular weight of 4 kD. TRITC-dextran MW 4000 exhibits an excitation wavelength of 555 nm. TRITC-dextran MW 4000 is vessel penetrate, which could label blood plasma to visualize the vasculature. TRITC-dextran MW 4000 is utilized in drug delivery for the stability of TRITC over a wide pH range (i.e. pH 2–11) and resistance to photo-bleaching .
    TRITC-dextran, MW 4000
  • HY-158082A
    TRITC-dextran, MW 20000

    Tetramethyl rhodamine isothiocyanate glucan, MW 20000

    		 Fluorescent Dye Others
    TRITC-dextran, MW 20000 (Tetramethyl rhodamine isothiocyanate glucan, MW 20000) is a fluorescent dye, with the molecular weight of 20 kD. TRITC-dextran MW 20000 exhibits an excitation wavelength of 555 nm. TRITC-dextran MW 20000 is vessel penetrate, which could label blood plasma to visualize the vasculature. TRITC-dextran MW 20000 is utilized in drug delivery for the stability of TRITC over a wide pH range (i.e. pH 2–11) and resistance to photo-bleaching .
    TRITC-dextran, MW 20000
  • HY-158082B
    TRITC-dextran, MW 40000

    Tetramethyl rhodamine isothiocyanate glucan, MW 40000

    		 Fluorescent Dye Others
    TRITC-dextran, MW 40000 (Tetramethyl rhodamine isothiocyanate glucan, MW 40000) is a fluorescent dye, with the molecular weight of 40 kD. TRITC-dextran MW 40000 exhibits an excitation wavelength of 555 nm. TRITC-dextran MW 40000 is vessel penetrate, which could label blood plasma to visualize the vasculature. TRITC-dextran MW 40000 is utilized in drug delivery for the stability of TRITC over a wide pH range (i.e. pH 2–11) and resistance to photo-bleaching .
    TRITC-dextran, MW 40000
  • 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-169064
    HIV-1 inhibitor-75

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor, with an EC50 value ranging from 0.0039 to 0.338 μM. The binding target of HIV-1 inhibitor-75 is reverse transcriptase, with an IC50 value of 0.055 μM. HIV-1 inhibitor-75 shows good in vitro metabolic stability, exhibiting moderate clearance rates and a longer half-life in human plasma and liver microsomes .
    HIV-1 inhibitor-75
  • HY-170368
    3′-Me Meayamycin D

    		SF3B1 Cancer
    3’-Me Meayamycin D is a splicing modulator on SF3B1 and PHF5A, that affects the pre-mRNA splicing process, and downregulates the MCL-1 expression. 3’-Me Meayamycin D inhibits the proliferation of cancer cell HCT116, SW48, A549, DMS53 and DMS114 with GI50 of 4.6-7.2 nM. 3’-Me Meayamycin D exhibits good plasma stability in mice with a halt-life of 16 h .
    3′-Me Meayamycin D
  • HY-P2161
    TAK-683

    		Kisspeptin Receptor Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
    TAK-683
  • HY-P2161B
    TAK-683 acetate
    1 Publications Verification

    		 Kisspeptin Receptor Cancer
    TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
    TAK-683 acetate
  • HY-P2161A
    TAK-683 TFA

    		Kisspeptin Receptor Cancer
    TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
    TAK-683 TFA
  • HY-161823
    Anti-MRSA agent 13

    		Bacterial Infection
    Anti-MRSA agent 13 (Compound 9b) is an agent against methicillin-resistant Staphylococcus aureus (MRSA), exhibiting a minimum inhibitory concentration (MIC) of 0.5–2 μg/mL against clinically isolated MRSA strains. Anti-MRSA agent 13 possesses favorable biosafety, plasma tolerance stability, and a low tendency to develop resistance. Anti-MRSA agent 13 disrupts cell walls and membranes, reduces metabolic activity, causes oxidative damage, affects DNA function, and ultimately leads to MRSA death through multi-target synergies .
    Anti-MRSA agent 13
  • HY-160023
    D3S-001

    		Ras Cancer
    D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 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 .
    D3S-001
  • HY-159563
    Mal-va-mac-SN38

    		Drug-Linker Conjugates for ADC Cancer
    Mal-va-mac-SN38 is a drug-linker conjugate for ADC. Mal-va-mac-SN38 contains a ADC cytotoxin SN-38 (HY-13704) and a linker (HY-126364). Mal-va-mac-SN38 can rapidly and covalently bind with endogenous albumin in vivo, resulting in the formation of HSA-va-mac-SN38. Mal-va-mac-SN38 demonstrates exceptional stability in human plasma, and has anti-tumor and anti-metastasis effect .
    Mal-va-mac-SN38
  • HY-163783
    CSNK2-IN-1

    		Casein Kinase Infection
    CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
    CSNK2-IN-1

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