Search Result
Results for "
plasma half-life
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-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-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-P99397
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ALX 0761; M 1095
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Interleukin Related
MMP
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Inflammation/Immunology
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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 .
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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-121307
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Drug Derivative
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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-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-156188
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Cholinesterase (ChE)
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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-173066
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PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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NU227326 is the PROTAC degrader for Indoleamine 2,3-dioxygenase 1 (IDO1) with DC50 of 4.5 nM. NU227326 degrades IDO1 in cell U87 and GBM43 with DC50 of 7.1 nM and 11.8 nM. NU227326 exhibits good pharmacokinetic properties with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours .(Pink: ligand for target protein IDO1 ligand-1 (HY-173067); Black: linker (HY-173068); Blue: ligand for E3 ligase Cereblon (HY-W087383))
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- HY-17421
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TU-199
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Proton Pump
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Infection
Inflammation/Immunology
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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 .
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- HY-116790B
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(Rac)-Penbutolol; (±)-Isopenbutolol
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Adrenergic Receptor
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Cardiovascular Disease
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(±)-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 .
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- HY-156404
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Fluorescent Dye
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Others
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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 .
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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-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-152142
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JNK
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Neurological Disease
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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 .
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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-121814A
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(R)-Acenocoumarin; (R)-Nicoumalone
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VD/VDR
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Cardiovascular Disease
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(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.
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- HY-172090
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Ser/Thr Protease
Potassium Channel
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Inflammation/Immunology
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MASP-2-IN-1 (Compound 77) is the inhibitor for mannan-binding lectin-associated serine protease (MASP), that inhibits MASP2 and MASP3 with IC50 of 11.4 nM and 13.2 µM. MASP-2-IN-1 exhibits a weak inhibitory activity against hERG with an IC50 of 175 µM. MASP-2-IN-1 reveals a poor stability in mouse plasma with a half-life of 4.4 hours .
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- HY-169064
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HIV
Reverse Transcriptase
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Infection
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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 .
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- HY-120623
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Na+/H+ Exchanger (NHE)
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Neurological Disease
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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. .
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- HY-12594
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ABT-450; Veruprevir
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HCV Protease
HCV
SARS-CoV
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Infection
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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) .
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- HY-164477
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Androgen Receptor
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Cancer
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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) .
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- HY-12594A
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ABT-450 dihydrate; Veruprevir dihydrate
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HCV Protease
HCV
SARS-CoV
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Infection
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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) .
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- HY-176019
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p38 MAPK
c-Myc
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Cardiovascular Disease
Cancer
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Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy .
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- HY-162484
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SARS-CoV
Virus Protease
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Infection
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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 .
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- HY-164049
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Prostaglandin Receptor
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Inflammation/Immunology
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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 .
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- HY-158122
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DNA-PK
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Cancer
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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) .
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- HY-158118
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DNA-PK
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Cancer
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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) .
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Cat. No. |
Product Name |
Type |
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- HY-156404
-
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Dyes
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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 .
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Cat. No. |
Product Name |
Target |
Research Area |
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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-P4070
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Peptides
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Metabolic Disease
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Insulin icodec is an Insulin (HY-P0035) analog that strongly but reversibly binds to albumin. Insulin icodec has long plasma half-life. Insulin icodec can be used for the research of type 2 diabetes .
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- HY-P1838
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Peptides
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Cardiovascular Disease
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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 .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99671
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M-6495
|
ADAMTS
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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 .
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- HY-P99397
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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 .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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