Search Result
Results for "
plasma stability
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-41189
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ADC Linker
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Cancer
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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 .
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- HY-P6053
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-143255
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Phosphodiesterase (PDE)
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Cancer
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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 .
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- HY-13611
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BN 80915
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Topoisomerase
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Cancer
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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 .
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- HY-163004
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Trk Receptor
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Cancer
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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 .
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- HY-150681
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SARS-CoV
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Infection
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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 .
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- HY-107749
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- HY-150719
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Others
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Cancer
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AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM .
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- HY-163291
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Bacterial
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Infection
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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 .
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- HY-100432
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LOC14
2 Publications Verification
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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 .
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- HY-160031
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GLP Receptor
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Metabolic Disease
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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 .
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- HY-156188
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Others
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Others
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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 .
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- HY-145842
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Virus Protease
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Infection
Neurological Disease
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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 .
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- HY-155047
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Bacterial
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Infection
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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 .
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- HY-126254
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BI-4924
1 Publications Verification
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Phosphoglycerate Dehydrogenase (PHGDH)
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Cancer
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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 .
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- HY-153715
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Mitochondria modulator-1
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Biochemical Assay Reagents
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Metabolic Disease
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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 .
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- HY-155011
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Others
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Others
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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 .
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- HY-143458
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FAK
PROTACs
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Cancer
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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 .
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- HY-163289
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Others
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Inflammation/Immunology
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TSLP binder-1 (compound 46) is a bicyclic peptide, which binds to thymic stromal lymphopoietin (TSLP) at the site used by IL-7Rα subunit, shows high affinity for TSLP, with KD of 13 nM. TSLP binder-1 reveals good stability in rat plasma and rat lung S9 fraction .
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- HY-147547
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Amyloid-β
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Neurological Disease
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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 .
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- HY-161247
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5-HT Receptor
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Metabolic Disease
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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 .
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- HY-163403
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VEGFR
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Cardiovascular Disease
Cancer
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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 .
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- HY-144771
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SARS-CoV
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Infection
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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 .
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- HY-144772
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SARS-CoV
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Infection
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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 .
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- HY-144770
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SARS-CoV
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Infection
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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 .
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- HY-128943
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Drug-Linker Conjugates for ADC
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Cancer
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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 .
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- HY-143877
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HDAC
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Cancer
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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) .
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- HY-158082
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Tetramethyl rhodamine isothiocyanate glucan, MW 4000
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Fluorescent Dye
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Others
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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 .
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- HY-158082A
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Tetramethyl rhodamine isothiocyanate glucan, MW 20000
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Fluorescent Dye
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Others
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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 .
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- HY-158082B
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Tetramethyl rhodamine isothiocyanate glucan, MW 40000
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Fluorescent Dye
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Others
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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 .
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- HY-P2161
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Kisspeptin Receptor
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Cancer
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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 .
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- HY-P2161B
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Kisspeptin Receptor
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Cancer
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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 .
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- HY-P2161A
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Kisspeptin Receptor
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Cancer
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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 .
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Cat. No. |
Product Name |
Type |
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- HY-158082
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Tetramethyl rhodamine isothiocyanate glucan, MW 4000
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Cell Assay Reagents
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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 .
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- HY-158082A
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Tetramethyl rhodamine isothiocyanate glucan, MW 20000
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Cell Assay Reagents
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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 .
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- HY-158082B
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Tetramethyl rhodamine isothiocyanate glucan, MW 40000
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Cell Assay Reagents
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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 .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2161B
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Kisspeptin Receptor
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Cancer
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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 .
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- HY-P6053
-
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Opioid Receptor
|
Neurological Disease
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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 .
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- HY-P2161
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Kisspeptin Receptor
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Cancer
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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 .
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- HY-P2161A
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Kisspeptin Receptor
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Cancer
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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 .
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