Search Result
Results for "
Half-life.
" in MedChemExpress (MCE) Product Catalog:
33
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-121243
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Herbicide
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Others
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Halauxifen is a herbicide with plasma elimination half-life of 1 h .
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- HY-129230
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Endogenous Metabolite
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Cardiovascular Disease
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Triletide is a thromboxane A2 antagonist with good oral absorption activity. The biotransformation of Triletide mainly includes the formation of demethyl, deacetyl, demethyl-deacetyl and hydroxy derivatives. The distribution half-life of Triletide is about 1 hour, and the elimination half-life is about 5 hours .
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- HY-120374
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Others
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Metabolic Disease
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V-PYRRO/NO is a NO donor in vivo. Following hepatic metabolism, it spontaneously decomposes with a half-life of 3 seconds to liberate NO.
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- HY-W743988
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Antibiotic
Bacterial
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Infection
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Cilastatin ammonium salt is an antibiotic that is relatively effective against Gram-positive cocci with a half-life of 3-4 h .
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- HY-114663
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Cannabinoid Receptor
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Others
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FDU-PB-22 is a new synthetic cannabinoid that is rapidly metabolized in HLM, with a half-life of 12.4 minutes .
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- HY-158395
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YAP
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Cancer
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TEAD-IN-13 (64) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 3.2 h in mouse .
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- HY-158396
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YAP
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Cancer
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TEAD-IN-14 (75a) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 2.3 h in mouse .
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- HY-158394
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YAP
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Cancer
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TEAD-IN-12 (58B) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 3.6 h in mouse .
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- HY-P99478
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IFNAR
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Inflammation/Immunology
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Bifarcept is a recombinant antibody of interferon receptor type I (IFN-RI). Bifarcept can bind IFN-β and prolong its serum half-life .
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- HY-121307
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Others
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Metabolic Disease
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Gliamilide is an active and well tolerated sulfamylurea derivative and displays a very short plasma half-life. Gliamilide is promising for research of maturity-onset diabetic deseases .
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- HY-163683
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Drug-Linker Conjugates for ADC
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Cancer
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EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .
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- HY-10758
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Factor Xa
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Cardiovascular Disease
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FXa-IN-1 is a FXa inhibitor (IC50: 3 nM, Ki: 0.7 nM) with respectable oral bioavailability and half-life in vivo. FXa-IN-1 can be used for thromboembolic disorders .
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- HY-103501
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GABA Receptor
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Neurological Disease
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SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .
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- HY-169127
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5-HT Receptor
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Neurological Disease
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Seganserin is an orally active 5-HT receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research .
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- HY-145362
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LPL Receptor
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Others
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S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
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- HY-137270
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- HY-135842
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Bacterial
Antibiotic
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Infection
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Aspoxicillin is a broad-spectrum antimicrobial agent against 68 isolates of Actinobacillus pleuropneumoniae with an MIC90 value of <= 0.05 μg/ml. Aspoxicillin has a long half-life in mouse serum of 55 minutes .
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- HY-148571
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- HY-14834
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- HY-135226
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Others
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Others
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PROLI NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 1.8 seconds at 37°C (pH 7.4) to liberate 2 moles of NO per mole of parent compound.
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- HY-B1300A
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Others
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Others
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Pharmacokinetic studies of Cefonicid have shown that high blood concentrations can be achieved rapidly after intravenous and intramuscular injection, and that concomitant use of albendazole prolongs its half-life in the body and reduces the rate of renal excretion .
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- HY-118561
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AD-1590
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Others
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Inflammation/Immunology
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Bermoprofen (AD-1590) is an orally active non-steroidal anti-inflammatory agent. Bermoprofen has potent antipyretic activities with a short biological half-life. Bermoprofen is a potent antagonist of LPS-induced fever in rabbits .
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- HY-W440699
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-acid (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-acid (MW 3400) can be used in drug delivery research .
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- HY-W440700
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-acid (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-acid (MW 5000) can be used in drug delivery research .
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- HY-W591891
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-acid (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-acid (MW 1000) can be used in drug delivery research .
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- HY-B1300B
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Others
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Others
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Pharmacokinetic studies of Cefonicid monosodium have shown that high blood concentrations can be achieved rapidly after intravenous and intramuscular injection, and that concomitant use of albendazole prolongs its half-life in the body and reduces the rate of renal excretion .
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- HY-125301
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Others
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Inflammation/Immunology
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Thymoctonan (THF-γ2) is the immunomodulatory octapeptide, thymic humoral factor γ2. Thymoctonan has the half-life less than 6 min at 37 °C in blood from human, rat and mouse .
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- HY-W394903
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JAK
Drug Metabolite
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Cancer
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GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
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- HY-P99671
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M-6495
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ADAMTS
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Inflammation/Immunology
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Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
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- HY-N4009
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Others
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Others
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Iriflophenone 2-O-α-rhamnoside can be isolated from the leaves of Aquilaria sinensis. Iriflophenone 2-O-α-rhamnoside has a half-life value of 2.44 min in rats at the administration of 25 mg/kg .
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- HY-167856
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GPR88
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Neurological Disease
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RTI-122 is a brain-penetrant and potent GPR88 agonist with good metabolic stability (half-life of 5.8 h in mice) and a cAMP EC50 of 11 nM. RTI-122 can be utilized in research on excessive drinking .
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- HY-164891
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Molecular Glues
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Others
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EM12-FS is a cereblon (CRBN) ligand that binds CRBN at His353 and a molecular glue degrader of NTAQ1. EM12-FS has a human plasma half-life of 196 min .
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- HY-134636
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Endogenous Metabolite
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Endocrinology
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PAPA NONOate is a NO donor with a NO release half-life of 77 min (22-25°C). PAPA NONOate may represent a potential research for impaired wound healing in diabetes by increasing the rate of collagen synthesis at the wound site .
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- HY-127128
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ACC-9089 sulfate
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Adrenergic Receptor
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Neurological Disease
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Flestolol (ACC-9089) sulfate is a competitive, ultra-short-acting beta-adrenergic blocking agent. Flestolol sulfate shows a half-life of approximately 6.5 minutes. Flestolol sulfate has the potential for the research of chest pain .
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- HY-W440704
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-NHS (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 5000) can be used in drug delivery research .
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- HY-W440689
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-amine (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-amine (MW 1000) can be used in drug delivery research .
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- HY-W440691
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-amine (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-amine (MW 3400) can be used in drug delivery research .
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- HY-W440692
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-amine (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-amine (MW 5000) can be used in drug delivery research .
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- HY-W440693
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-azide (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-azide (MW 1000) can be used in drug delivery research .
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- HY-W440695
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-azide (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-azide (MW 3400) can be used in drug delivery research .
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- HY-W440696
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-azide (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-azide (MW 5000) can be used in drug delivery research .
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- HY-W440697
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-NHS (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 1000) can be used in drug delivery research .
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- HY-W440702
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-NHS (MW 2000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 2000) can be used in drug delivery research .
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- HY-W440703
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-NHS (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 3400) can be used in drug delivery research .
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- HY-W440705
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-alcohol (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 1000) can be used in drug delivery research .
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- HY-W440707
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-alcohol (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 3400) can be used in drug delivery research .
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- HY-W440708
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-alcohol (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 5000) can be used in drug delivery research .
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- HY-W440709
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-alcohol (MW 10000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 10000) can be used in drug delivery research .
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- HY-W440710
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Biotin (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Biotin (MW 1000) can be used in drug delivery research .
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- HY-W440712
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Biotin (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Biotin (MW 3400) can be used in drug delivery research .
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- HY-W440713
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Biotin (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Biotin (MW 5000) can be used in drug delivery research .
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- HY-W440714
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Folate (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Folate (MW 1000) can be used in drug delivery research .
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- HY-W440716
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Folate (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Folate (MW 3400) can be used in drug delivery research .
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- HY-W440717
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Folate (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Folate (MW 5000) can be used in drug delivery research .
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- HY-W440718
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Mal (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Mal (MW 1000) can be used in drug delivery research .
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- HY-W440720
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Mal (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Mal (MW 3400) can be used in drug delivery research .
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- HY-W440721
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Mal (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Mal (MW 5000) can be used in drug delivery research .
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- HY-W440723
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Thiol (MW 2000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Thiol (MW 2000) can be used in drug delivery research .
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- HY-W440725
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Thiol (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Thiol (MW 5000) can be used in drug delivery research .
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- HY-W440726
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Vinylsulfone (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Vinylsulfone (MW 1000) can be used in drug delivery research .
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- HY-W440728
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Vinylsulfone (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Vinylsulfone (MW 3400) can be used in drug delivery research .
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- HY-W440729
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-Vinylsulfone (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Vinylsulfone (MW 5000) can be used in drug delivery research .
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- HY-W591912
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-methoxy (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-methoxy (MW 1000) can be used in drug delivery research .
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- HY-W591914
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Biochemical Assay Reagents
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Others
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Cholesterol-PEG-methoxy (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-methoxy (MW 5000) can be used in drug delivery research .
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- HY-153027
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Methylergonovine; Ryegonovin free base; Spametrin F free base
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5-HT Receptor
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Endocrinology
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Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. The distribution half-life of Methylergometrine is only 1-2 min. Methylergometrine can be used as an oxytocin to treat uterine atony .
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- HY-W507393
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DPTA-NO
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Biochemical Assay Reagents
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Others
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Dipropylenetriamine NONOate (DPTA-NO) is a NO donor, which spontaneously dissociates in a pH-dependent, first-order process with a half-life of three hours and five hours at 37°C and 22-25°C, pH 7.4, respectively .
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- HY-163505
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Bacterial
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Others
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Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
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- HY-139347
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- HY-163438
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- HY-100607A
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ONO1101 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist .
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- HY-P99350
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AMG 910; Anti-Human CD3xClaudin18 2
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CD3
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Cancer
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Gresonitamab (AMG 910) is a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody targets CD3-positive T cells and CLDN18.2-expressing tumor cells. Gresonitamab can be used for the research of adenocarcinoma .
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- HY-100607
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- HY-N7122
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Endogenous Metabolite
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Inflammation/Immunology
Cancer
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Thymopentin is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
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- HY-N7122A
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Endogenous Metabolite
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Inflammation/Immunology
Cancer
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Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
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- HY-124713
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DNA/RNA Synthesis
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Neurological Disease
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ML372 inhibits survival motor neuron (SMN) protein ubiquitination, increases SMN protein stability without affecting mRNA expression. ML372 improves spinal muscular atrophy (SMA) in mice. ML372 is brain penetrant and has a reasonable exposure and half-life in vivo .
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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-135842R
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Bacterial
Antibiotic
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Infection
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Aspoxicillin (Standard) is the analytical standard of Aspoxicillin. This product is intended for research and analytical applications. Aspoxicillin is a broad-spectrum antimicrobial agent against 68 isolates of Actinobacillus pleuropneumoniae with an MIC90 value of <= 0.05 μg/ml. Aspoxicillin has a long half-life in mouse serum of 55 minutes .
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- HY-P99930
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FGFR
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Metabolic Disease
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Efruxifermin is an Fc-FGF21 fusion protein (human IgG1 Fc domain linked to a modified human FGF21). Efruxifermin has prolonged half-life and enhanced receptor affinity compared with native human FGF21. Efruxifermin can be used for the research of non-alcoholic steatohepatitis .
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- HY-13859
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L-FMAU
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HBV
DNA/RNA Synthesis
Orthopoxvirus
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Infection
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Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
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- HY-P10019
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NLY01
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GCGR
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Neurological Disease
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Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
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- HY-14466
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Prostaglandin Receptor
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Endocrinology
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GW 848687X is a selective, orally active prostaglandin EP1 receptor antagonist for the inhibition of inflammatory pain. The oral bioavailability of GW 848687X was 54% in rats and 53% in dogs. GW 848687X has a half-life of 2 hours and has inhibitory potential for both acute and chronic pain .
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- HY-W739302
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Sodium α-oxyhyponitrite
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Others
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Others
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Sodium Oxyhyponitrite Angeli (Angeli) is a nitroxyl (NO-) donor, but under certain conditions NO release has also been observed. Sodium Oxyhyponitrite Angeli spontaneously dissociates in a pH-dependent first-order process with a half-life of 2.3 minutes at 37°C (pH 7.4), releasing 0.54 mol NO per mole.
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- HY-100658
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic agent candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor .
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- HY-155507
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c-Myc
|
Cancer
|
|
c-Myc inhibitor 11 (Compound 67e) is a c-MYC inhibitor (pEC50: 6.4). c-Myc inhibitor 11 has high clearance levels, moderate volume of distribution and short half-life in rat pharmacokinetic assay. c-Myc inhibitor 11 can be used for cancer research .
|
-
- HY-162351
-
|
|
Others
|
Metabolic Disease
|
|
EBP-IN-1 (compound 11) is an inhibitor of emopamil-binding protein (EBP), a sterol isomerase in the cholesterol biosynthetic pathway. EBP-IN-1 has a long half-life in rodents and has good metabolic turnover and brain penetration properties. EBP-IN-1 enhances oligodendrocyte formation in human cortical organoids .
|
-
- HY-111186
-
|
WL 108366
|
Glucocorticoid Receptor
MMP
|
Others
|
|
Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects .
|
-
- HY-121246
-
|
AKF-PD
|
PI3K
Akt
|
Inflammation/Immunology
|
|
Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway .
|
-
- HY-100607AR
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Landiolol (hydrochloride) (Standard) is the analytical standard of Landiolol (hydrochloride). This product is intended for research and analytical applications. Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist .
|
-
- HY-17421
-
|
TU-199
|
Proton Pump
|
Infection
Inflammation/Immunology
|
|
Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H +/K +-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV .
|
-
- HY-B1118S1
-
|
RP-14539-13C2, 15N2; PM-185184-13C2, 15N2
|
Isotope-Labeled Compounds
Parasite
Antibiotic
|
Infection
|
|
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
|
-
- HY-149014
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
|
-
- HY-P99397
-
|
ALX 0761; M 1095
|
Interleukin Related
MMP
|
Inflammation/Immunology
|
|
Sonelokimab (ALX 0761) is a trivalent bispecific nanobody composed of camel derived humanized IL-17F antibodies, IL-17A/F antibodies, and serum albumin VHH antibodies. Sonelokimab can prolong the plasma half-life by binding to human serum albumin. Sonelokimab can be used for research on rheumatoid arthritis and psoriasis .
|
-
- 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 .
|
-
- HY-132242
-
|
SFN-NAC
|
HDAC
Apoptosis
Drug Metabolite
|
Cancer
|
|
DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC) is an orally active HDAC inhibitor and metabolite of sulforaphane (HY-13755) with longer half-life and better blood-brain barrier permeability. DL-Sulforaphane N-acetyl-L-cysteine activates autophagy-mediated downregulation of α-tubulin expression through the ERK pathway and can be used in cancer research .
|
-
- HY-145969A
-
|
|
Others
|
Cancer
|
|
β-S-ARCA (triammonium) is a mRNA 7-methylguanosine (m 7G) cap analog carrying a phosphorothioate (PS) moiety. mRNA incorporating β-S-ARCA (triammonium) can prolong cellular half-life and increase protein expression. β-S-ARCA (triammonium) can be used in research of mRNA-based anti-cancer vaccines .
|
-
- HY-P99814
-
|
AMG-701
|
CD3
|
Inflammation/Immunology
Cancer
|
|
Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) .
|
-
- HY-158991
-
|
|
CFTR
|
Inflammation/Immunology
|
|
I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents .
|
-
- HY-105110
-
|
SM-8668
|
Fungal
|
Infection
|
|
SM-8668 is an effective orally active antifungal agent, with median effective doses (ED50) of 0.18, 3.7, and 5.9 mg/kg for systemic candidiasis, aspergillosis, and cryptococcosis in mice, respectively. Pharmacokinetic studies in mice and rats indicate that SM-8668 has a long half-life and a high total exposure. SM-8668 can be used in anti-infective research .
|
-
- HY-168595
-
|
|
Casein Kinase
|
Infection
|
|
CSNK2-IN-2 (compound 2) is an orally active CSNK2 inhibitor. CSNK2-IN-2 has an IC50 of 29 μM against CLK11. CSNK2-IN-2 has a half-life of 2.5 h and an AUC of 10,100 h × nM. CSNK2-IN-2 can be used in antiviral studies .
|
-
- HY-135774
-
|
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an anti-angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting .
|
-
- HY-162940
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC50s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .
|
-
- HY-147336
-
|
|
Drug Metabolite
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
|
-
- HY-124209
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
9-keto Fluprostenol is an analog of prostaglandin E2 (PGE2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-9 of fluprostenol yields 9-keto fluprostenol. It is anticipated that this analog will have strong affinity for EP receptors and act as a PGE2 agonist.
|
-
- HY-111186R
-
|
|
Glucocorticoid Receptor
MMP
|
Others
|
|
Flocoumafen (Standard) is the analytical standard of Flocoumafen. This product is intended for research and analytical applications. Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects .
|
-
- HY-144771
-
|
|
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 .
|
-
- HY-144772
-
|
|
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 .
|
-
- HY-144770
-
|
|
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 .
|
-
- HY-P99340
-
|
VIR 7831
|
SARS-CoV
|
Infection
Cancer
|
|
Sotrovimab (VIR 7831) is a human IgG1κ pan-sarbecovirus monoclonal antibody (mAb), neutralizes SARS-CoV-2, SARS-CoV-1, and multiple other sarbecoviruses. Sotrovimab is developed based on S309, exhibits a long half-life and great bioavailability in the respiratory mucosa. Sotrovimab could result in immune-mediated viral clearance and prevent progression of Covid-19 early in the course of disease .
|
-
- HY-152142
-
|
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
|
-
- HY-155974
-
|
|
MDM-2/p53
|
Cancer
|
|
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction .
|
-
- HY-107129
-
|
|
GCGR
|
Metabolic Disease
|
|
MK-3577 is an orally effective glucagon receptor (GCGR) antagonist that reduces hepatic glucose production and lowers blood glucose levels by blocking glucagon receptors on target organs, primarily the liver. Pharmacokinetic analysis in domestic cats indicates that MK-3577 reaches peak levels 3 to 4 hours after oral administration, with a half-life of approximately 15 hours. MK-3577 can be used in diabetes research .
|
-
- HY-162583
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
|
-
- HY-117482
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-117482A
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-P3347
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (Ki=5.7 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life .
|
-
![NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)](//file.medchemexpress.eu/product_pic/hy-p3347.gif)
- HY-169064
-
|
|
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 .
|
-
- HY-116790B
-
|
(Rac)-Penbutolol; (±)-Isopenbutolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
(±)-Penbutolol ((Rac)-Penbutolol) is the racemic mixture of Penbutolol. (±)-Penbutolol is an orally active β-adrenergic receptor antagonist. (±)-Penbutolol antagonizes exercise-induced tachycardia, reduces the increase in peak expiratory flow rate (PEFR) caused by exercise, and decreases resting plasma renin activity (PRA). (±)-Penbutolol reaches peak plasma concentration 1 hour after oral administration, with a half-life of 4.5 hours, and is converted into an active metabolite in the body. (±)-Penbutolol can be used in cardiovascular-related disease research .
|
-
- HY-W762012
-
|
OCDD
|
Cytochrome P450
|
Others
|
|
Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant but is not acutely toxic. In rats, Octachlorodibenzo-p-dioxin (50 μg/kg i.v. or 50-5000 μg/kg p.o.) has a systemic elimination half-life of 3-5 months and accumulates and concentrates in the liver and adipose tissue after low-dose, repeated exposure. Repeated administration of octachlorodibenzo-p-dioxin causes increases in 7-ethoxyresorufin-O-deethylase (7-EROD) activity and total cytochrome P-450 levels .
|
-
- HY-156404
-
|
|
Fluorescent Dye
|
Others
|
|
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
|
-
- HY-126911
-
|
Fluprostenol Prostaglandin D2
|
Prostaglandin Receptor
|
Endocrinology
|
|
11-keto Fluprostenol is an analog of prostaglandin D2 (PGD2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-11 of fluprostenol yields 11-keto fluprostenol. 11-keto Fluprostenol exhibits moderate binding to the CRTH2/DP2 receptor compared to PGD2 and essentially no activity at the DP1 receptor.
|
-
- HY-120812
-
|
|
HIV Protease
|
Infection
|
|
HIV-IN-11 is part of the hydroxylaminoglutaramide (HAPA) transition state isomeric series of HIV protease inhibitors and is a potent and selective inhibitor of HIV-1 protease. HIV-IN-11 competitively inhibits HIV-1 PR (Ki: 0.049 nM) and potently inhibits replication of HIV(IIIb)-infected MT4 lymphocytes at concentrations of 25.0-50.0 nM. HIV-IN-11 displays a longer half-life than indinavir sulfate in animal models and serves as a promising second-generation HIV protease inhibitor .
|
-
- HY-14308
-
|
PSI-7851
|
Endogenous Metabolite
|
Infection
|
|
GS-9851 (PSI-7851) is an HCV nonstructural protein 5B (NS5B) inhibitor with potential activity for the treatment of HCV infection. GS-9851 showed good tolerability in patients with initial HCV genotype 1 infection. GS-9851 is rapidly cleared from the body with a half-life of approximately 1 hour. The maximum concentration of GS-9851 and the increase in the area under the compound concentration-time curve were not dose-proportional, especially at the highest dose .
|
-
- HY-123446
-
|
|
Others
|
Neurological Disease
|
|
JNJ-42259152 is a phosphodiesterase 10A (PDE10A) positron emission tomography (PET) tracer that is specific for PDE10A activity. JNJ-42259152 can be dynamically scanned in healthy volunteers to assess its kinetic properties in the brain. The half-life of JNJ-42259152 in the blood is an average of 90 minutes. JNJ-42259152 has demonstrated reliable binding potential (BPND) in different target areas (such as the lentiform nucleus, caudate nucleus, ventral striatum, etc.), providing an important tool for studying neuropsychiatric diseases .
|
-
- HY-12594
-
Paritaprevir
Maximum Cited Publications
12 Publications Verification
ABT-450; Veruprevir
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
|
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
|
-
- HY-108251
-
|
DAMPA
|
Antifolate
Drug Metabolite
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
Inflammation/Immunology
|
|
Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation .
|
-
- HY-121814A
-
|
(R)-Acenocoumarin; (R)-Nicoumalone
|
VD/VDR
|
Cardiovascular Disease
|
|
(R)-Acenocoumarol ((R)-Acenocoumarin; (R)-Nicoumalone) is a short-acting and orally active anticoagulant, like Warfarin (HY-B0687), works by inhibiting vitamin K epoxide reductase. (R)-Acenocoumarol has a greater in vivo anticoagulant potency than Warfarin. (R)-Acenocoumarol has a single chiral center that produces two different enantiomeric forms. (R)-Acenocoumarol has a longer plasma elimination half-life (6.6 h) and a slower plasma clearance rate (1.9 L/h) than the (S)-enantiomer, resulting in a stronger in vivo anticoagulant effect.
|
-
- HY-120623
-
|
|
Na+/H+ Exchanger (NHE)
|
Neurological Disease
|
|
BMS-284640 is a synthetic sodium hydrogen exchange isomer-1 (NHE-1) inhibitor. BMS-284640 has a more than 380-fold higher NHE-1 inhibitory activity (IC50: 9 nM) compared to cariporide (HY-19693) and is more selective for NHE-1 over NHE-2 (IC50: 1.8 μM) and NHE-5 (IC50: 3.36 μM). BMS-284640 and its analogs also exhibit enhanced oral bioavailability and prolonged plasma half-life in rats. .
|
-
- HY-159174
-
|
|
Ephrin Receptor
Cyclin G-associated Kinase (GAK)
Dengue virus
|
Infection
|
|
EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells .
|
-
- HY-12594A
-
|
ABT-450 dihydrate; Veruprevir dihydrate
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
|
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) .
|
-
- HY-164477
-
|
|
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) .
|
-
- HY-162484
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
GZNL-P36 is an orally active inhibitor for SARS-CoV-2 papain-like protease (PL pro), with an IC50 of 6.45 nM. GZNL-P36 inhibits SARS-CoV and its variants with EC50 range from 58.2 nM to 2.66 μM. GZNL-P36 exhibits a peak plasma concentration Cmax of 549 ng/mL, a half-life T1/2 of 1.45 h and a bioavailability of 74.7% in CD-1 mouse. GZNL-P36 exhibits antiviral activity in SARS-CoV-2 XXB.1 infection in mouse .
|
-
- HY-164049
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases .
|
-
- HY-168715
-
|
|
SHP2
Apoptosis
MAPKAPK2 (MK2)
|
Cancer
|
|
SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
|
-
- HY-169432
-
|
|
GABA Receptor
|
Neurological Disease
|
|
TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively) .
|
-
- HY-123022
-
|
CS-023; RO4908463; R-115685
|
Bacterial
|
Infection
|
|
Tomopenem (CS-023; RO4908463; R-115685) is a longer-half-life parenteral carbapenem. Tomopenem shows broad activity against 63 reference species. The activity of tomopenem against 293 clinical isolates is potent (MIC90, 0.06 to 4 μg/mL). Antianaerobic activity .
|
-
- HY-158122
-
|
|
DNA-PK
|
Cancer
|
|
Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
|
-
- HY-P99562
-
|
XmAb-18087
|
CD3
|
Cancer
|
|
Tidutamab (XmAb-18087) is a humanized and affinity-optimized bispecific antibody (bsAb) targeting SSTR2 binding domain and T-cell binding domain (CD3). Tidutamab possesses a full Fc domain to maintain long serum half-life.Tidutamab eliminates SSTR+ tumor cells by stimulating redirected T cellmediated cytotoxicity (RTcC) .
|
-
- HY-158118
-
|
|
DNA-PK
|
Cancer
|
|
Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
|
-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-156404
-
|
|
Dyes
|
|
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W440699
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-acid (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-acid (MW 3400) can be used in drug delivery research .
|
-
- HY-W440700
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-acid (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-acid (MW 5000) can be used in drug delivery research .
|
-
- HY-W591891
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-acid (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-acid (MW 1000) can be used in drug delivery research .
|
-
- HY-W440704
-
|
|
Carbohydrates
|
|
Cholesterol-PEG-NHS (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 5000) can be used in drug delivery research .
|
-
- HY-W440689
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-amine (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-amine (MW 1000) can be used in drug delivery research .
|
-
- HY-W440691
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-amine (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-amine (MW 3400) can be used in drug delivery research .
|
-
- HY-W440692
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-amine (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-amine (MW 5000) can be used in drug delivery research .
|
-
- HY-W440693
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-azide (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-azide (MW 1000) can be used in drug delivery research .
|
-
- HY-W440695
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-azide (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-azide (MW 3400) can be used in drug delivery research .
|
-
- HY-W440696
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-azide (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-azide (MW 5000) can be used in drug delivery research .
|
-
- HY-W440697
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-NHS (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 1000) can be used in drug delivery research .
|
-
- HY-W440702
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-NHS (MW 2000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 2000) can be used in drug delivery research .
|
-
- HY-W440703
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-NHS (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-NHS (MW 3400) can be used in drug delivery research .
|
-
- HY-W440705
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-alcohol (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 1000) can be used in drug delivery research .
|
-
- HY-W440707
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-alcohol (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 3400) can be used in drug delivery research .
|
-
- HY-W440708
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-alcohol (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 5000) can be used in drug delivery research .
|
-
- HY-W440709
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-alcohol (MW 10000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-alcohol (MW 10000) can be used in drug delivery research .
|
-
- HY-W440710
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Biotin (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Biotin (MW 1000) can be used in drug delivery research .
|
-
- HY-W440712
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Biotin (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Biotin (MW 3400) can be used in drug delivery research .
|
-
- HY-W440713
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Biotin (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Biotin (MW 5000) can be used in drug delivery research .
|
-
- HY-W440714
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Folate (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Folate (MW 1000) can be used in drug delivery research .
|
-
- HY-W440716
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Folate (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Folate (MW 3400) can be used in drug delivery research .
|
-
- HY-W440717
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Folate (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Folate (MW 5000) can be used in drug delivery research .
|
-
- HY-W440718
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Mal (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Mal (MW 1000) can be used in drug delivery research .
|
-
- HY-W440720
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Mal (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Mal (MW 3400) can be used in drug delivery research .
|
-
- HY-W440721
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Mal (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Mal (MW 5000) can be used in drug delivery research .
|
-
- HY-W440723
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Thiol (MW 2000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Thiol (MW 2000) can be used in drug delivery research .
|
-
- HY-W440725
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Thiol (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Thiol (MW 5000) can be used in drug delivery research .
|
-
- HY-W440726
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Vinylsulfone (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Vinylsulfone (MW 1000) can be used in drug delivery research .
|
-
- HY-W440728
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Vinylsulfone (MW 3400) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Vinylsulfone (MW 3400) can be used in drug delivery research .
|
-
- HY-W440729
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-Vinylsulfone (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-Vinylsulfone (MW 5000) can be used in drug delivery research .
|
-
- HY-W591912
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-methoxy (MW 1000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-methoxy (MW 1000) can be used in drug delivery research .
|
-
- HY-W591914
-
|
|
Drug Delivery
|
|
Cholesterol-PEG-methoxy (MW 5000) is a cholesterol PEG derivative that can form micelles through molecular self-assembly and has a longer half-life in vivo. Cholesterol-PEG-methoxy (MW 5000) can be used in drug delivery research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-N7122
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Thymopentin is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
|
-
- HY-N7122A
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
|
-
- HY-P10274
-
|
|
Peptides
|
Inflammation/Immunology
|
|
CM05 is a bromo-fatty acid. CM05 can be used to modify ornithodoros moubata complement inhibitor (OmCI) and extend the half-life of OmCI .
|
-
- HY-P10019
-
|
NLY01
|
GCGR
|
Neurological Disease
|
|
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
|
-
- HY-P1838
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Proadrenomedullin (45-92), human, a mid-regional fragment of proadrenomedullin (MR-proADM), comprises amino acids 45–92 of pre-proADM. Proadrenomedullin (45-92), human has a longer half-life, is relatively stable and is produced in equimolar amounts to adrenomedullin (ADM), making it a surrogate for plasma levels of ADM gene products .
|
-
- HY-P3347
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (Ki=5.7 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life .
|
-
- HY-P10490
-
|
|
Peptides
|
Others
Cancer
|
|
(D-His(Bzl)6)-LHRH (1-7) free acid is a synthetic peptide compound that is a derivative of luteinizing hormone-releasing hormone (LHRH). (D-His(Bzl)6)-LHRH (1-7) free acid enhances its stability and biological activity by introducing unnatural amino acid residues at specific positions of the LHRH molecule. This modification can improve the drug's performance in the body half-life, reducing the rate at which it is rapidly metabolized and cleared, thereby enhancing its efficacy in inhibiting cell proliferation .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99671
-
|
M-6495
|
ADAMTS
|
Inflammation/Immunology
|
|
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
|
-
- HY-P99350
-
|
AMG 910; Anti-Human CD3xClaudin18 2
|
CD3
|
Cancer
|
|
Gresonitamab (AMG 910) is a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody targets CD3-positive T cells and CLDN18.2-expressing tumor cells. Gresonitamab can be used for the research of adenocarcinoma .
|
-
- HY-P99930
-
|
|
FGFR
|
Metabolic Disease
|
|
Efruxifermin is an Fc-FGF21 fusion protein (human IgG1 Fc domain linked to a modified human FGF21). Efruxifermin has prolonged half-life and enhanced receptor affinity compared with native human FGF21. Efruxifermin can be used for the research of non-alcoholic steatohepatitis .
|
-
- HY-P99397
-
|
ALX 0761; M 1095
|
Interleukin Related
MMP
|
Inflammation/Immunology
|
|
Sonelokimab (ALX 0761) is a trivalent bispecific nanobody composed of camel derived humanized IL-17F antibodies, IL-17A/F antibodies, and serum albumin VHH antibodies. Sonelokimab can prolong the plasma half-life by binding to human serum albumin. Sonelokimab can be used for research on rheumatoid arthritis and psoriasis .
|
-
- HY-P99814
-
|
AMG-701
|
CD3
|
Inflammation/Immunology
Cancer
|
|
Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) .
|
-
- HY-P99340
-
|
VIR 7831
|
SARS-CoV
|
Infection
Cancer
|
|
Sotrovimab (VIR 7831) is a human IgG1κ pan-sarbecovirus monoclonal antibody (mAb), neutralizes SARS-CoV-2, SARS-CoV-1, and multiple other sarbecoviruses. Sotrovimab is developed based on S309, exhibits a long half-life and great bioavailability in the respiratory mucosa. Sotrovimab could result in immune-mediated viral clearance and prevent progression of Covid-19 early in the course of disease .
|
-
- HY-P99478
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
Bifarcept is a recombinant antibody of interferon receptor type I (IFN-RI). Bifarcept can bind IFN-β and prolong its serum half-life .
|
-
- HY-P99562
-
|
XmAb-18087
|
CD3
|
Cancer
|
|
Tidutamab (XmAb-18087) is a humanized and affinity-optimized bispecific antibody (bsAb) targeting SSTR2 binding domain and T-cell binding domain (CD3). Tidutamab possesses a full Fc domain to maintain long serum half-life.Tidutamab eliminates SSTR+ tumor cells by stimulating redirected T cellmediated cytotoxicity (RTcC) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B1118S1
-
|
|
|
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-159174
-
|
|
|
Azide
|
|
EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-13859
-
|
L-FMAU
|
|
Nucleosides and their Analogs
|
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
|
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