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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
98 Results for "
plasma stability
" in MedChemExpress (MCE) Product Catalog:
Products (98)
98 Results for "plasma stability" in MCE Product Catalog:
5
5 Cited Publications
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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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4 Cited Publications
Cat. No.: HY-P2161B
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2
2 Cited Publications
Cat. No.: HY-158082
Synonyms: Tetramethyl rhodamine isothiocyanate glucan, MW 4000
2
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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1 Cited Publications
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BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
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1
1 Cited Publications
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MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
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1 Cited Publications
Cat. No.: HY-N0857
CAS No.: 79233-15-1
Cat. No.: HY-41189
CAS No.: 863971-53-3
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Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers .
Cat. No.: HY-160023
CAS No.: 2914919-85-8
Synonyms: D3S-001
Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
Cat. No.: HY-P10502
CAS No.: 2378836-93-0
Synonyms: (R)-VX-445
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(R)-Elexacaftor ((R)-VX-445) is the enantiomer of Elexacaftor (HY-111772). Elexacaftor is an orally active CFTR modulator that targets nucleotide-binding domain 1. Elexacaftor stabilizes misfolded F508del-CFTR protein, enhances its trafficking to the plasma membrane, and significantly improves metabolic stability, thermal stability and ion conductivity. Elexacaftor not only restores chloride transport function in nasal epithelial cells and rescues multiple CFTR mutation subtypes, but also exerts multiplicative synergistic effects with Ivacaftor (HY-13017), and is often used in a triple combination therapy with Tezacaftor (HY-15448). Elexacaftor is widely used in basic and clinical translational research on cystic fibrosis .
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ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively .
Cat. No.: HY-161247
CAS No.: 2641482-08-6
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5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
Cat. No.: HY-158082A
Synonyms: Tetramethyl rhodamine isothiocyanate glucan, MW 20000
Cat. No.: HY-175207
CAS No.: 3109469-27-1
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CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
Cat. No.: HY-W714524
CAS No.: 321863-21-2
Synonyms: 16:0-18:1 PS (POPS)
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1-Palmitoyl-2-oleoyl-sn-glycero-3-PS sodium (16:0-18:1 PS (POPS)) is an anionic phosphatidylserine phospholipid with 16:0 (palmitoyl) and 18:1 (oleoyl) acyl chains. It serves as a component of biomimetic inner plasma membrane models and membrane vesicles for hemostatic response studies. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PS sodium regulates membrane electrical properties by forming tethered bilayer lipid membranes. It enhances the stability of sHDL particles without altering the cholesterol efflux capacity of sHDL. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PS sodium acts synergistically with phosphatidylcholine to support prothrombin activation. It serves as a component of the 4:1 POPC/POPS binary lipid bilayer model. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PS sodium is applicable to research related to atherosclerosis .
Cat. No.: HY-P10502A
Cat. No.: HY-144734
CAS No.: 1024168-48-6
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Pantothenate kinase-IN-1 is a PANK3 inhibitor with an IC50 of 0.51 μM. Pantothenate kinase-IN-1 acts as a pantothenate-competitive inhibitor, which occupies the pantothenate-binding site of PANK3 and binds to both protomers in the PANK3 dimer. Pantothenate kinase-IN-1 exhibits metabolic stability in mouse and rat plasma. Pantothenate kinase-IN-1 can be used in the research of pantothenate kinase-associated neurodegenerative diseases and metabolic diseases .
Cat. No.: HY-W099504
CAS No.: 111-70-6
Synonyms: n-Heptyl alcohol
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
