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plasma clearance

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-119393
    Olanzapine N-oxide

    		Drug Metabolite Others
    Olanzapine N-oxide is a compound under investigation for the metabolism of antipsychotic compounds. Olanzapine N-oxidation and N-demethylation are catalyzed by different enzymes, and its plasma concentration and clearance are not affected by a single factor, such as a specific genotype or smoking behavior.
    Olanzapine N-oxide
  • HY-100432
    LOC14
    2 Publications Verification

    		 PDI Neurological Disease Inflammation/Immunology
    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding . LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
    LOC14
  • HY-116494A
    (6R)-ML753286

    		BCRP Cancer
    (6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
    (6R)-ML753286
  • HY-174375
    NEDD4-IN-1

    		Others Cancer
    NEDD4-IN-1 (Compound 32) is a potent inhibitor of NEDD4 (IC50 = 0.12 μM). NEDD4-IN-1 shows significant and comparable antiproliferative activity in H292 cell line. NEDD4-IN-1 demonstrates high plasma protein binding and medium-to-high in vitro clearance in both human and mouse models. NEDD4-IN-1 shows superior stability in mouse plasma. NEDD4-IN-1 has excellent potency, selectivity, and favourable in vitro ADME properties. NEDD4-IN-1 exhibits a systemic plasma clearance exceeding the hepatic blood flow in mouse model. NEDD4-IN-1 can be studied in anticancer research .
    NEDD4-IN-1
  • HY-143255
    Enpp-1-IN-11

    		Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
    Enpp-1-IN-11
  • HY-116494
    ML753286

    		BCRP Cancer
    ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
    ML753286
  • HY-156188
    AChE-IN-41

    		Cholinesterase (ChE) Others
    AChE-IN-41 (Compound 2) is a compound of the Galantamine Memantine hybrid. AChE-IN-41 has the inhibition ability of cholinesterase. AChE-IN-41 shows higher plasma stability and comparable microsomal stability in vitro, while showing lower half-life and faster clearance in vivo .
    AChE-IN-41
  • HY-162459
    cGAS-IN-3

    		Cyclic GMP-AMP Synthase Inflammation/Immunology
    cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats .
    cGAS-IN-3
  • HY-121814A
    (R)-Acenocoumarol

    (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.
    (R)-Acenocoumarol
  • HY-153993
    Pyrocatechol sulfate

    		Endogenous Metabolite Others
    Pyrocatechol sulfate, a phenolic metabolite present in human plasma, is associated with the consumption of specific foods such as berries and the condition of gut microbiota. It serves as a potential urinary biomarker for kidney function, dialytic clearance, whole grain consumption, and regular coffee intake. Additionally, Pyrocatechol sulfate, along with other phenolic sulfates, plays a role in modulating various biological functions, including those related to brain health and the rhythmic beating of cardiomyocytes.
    Pyrocatechol sulfate
  • HY-W241345
    DOTA-bis(tert-butyl)ester

    		Radionuclide-Drug Conjugates (RDCs) Cancer
    DOTA-bis(tert-butyl)ester is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide conjugates (RDCs). DOTA-bis(tert-butyl)ester can be conjugated with different salts to form different metal chelators, such as (HY-B1244) hydrochloride to obtain DOTA-MN2. DOTA-MN2 can be reacted with [67]Ga-citrate to obtain radiolabeling. When (67)Ga-DOTA-MN2 is incubated in phosphate buffer solution or mouse plasma for 24 hours, it does not undergo significant decomposition. In the biodistribution experiment of NFSa tumor mice, it has high tumor uptake and rapid plasma clearance, and is a good material for SPECT and PET studies.
    DOTA-bis(tert-butyl)ester
  • HY-169064
    HIV-1 inhibitor-75

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor, with an EC50 value ranging from 0.0039 to 0.338 μM. The binding target of HIV-1 inhibitor-75 is reverse transcriptase, with an IC50 value of 0.055 μM. HIV-1 inhibitor-75 shows good in vitro metabolic stability, exhibiting moderate clearance rates and a longer half-life in human plasma and liver microsomes .
    HIV-1 inhibitor-75
  • HY-117912
    TRC210258

    		Endogenous Metabolite Cardiovascular Disease
    TRC210258 is a TGR5 agonist with activity to improve diabetes-associated hyperglycemia and dyslipidemia. TRC210258 promotes energy expenditure by enhancing the release of glucagon-like peptide-1. TRC210258 is able to improve glucose metabolic control in high-fat diet-induced obese mice. TRC210258 also showed improvement in lipid parameters in high-fat-fed hamsters, including reductions in plasma triglyceride and low-density lipoprotein cholesterol levels. TRC210258 improved emerging lipid-related cardiovascular risk parameters including remnant cholesterol and triglyceride clearance .
    TRC210258
  • HY-N2263
    Skimmin
    1 Publications Verification

    Umbelliferone glucoside

    		 Interleukin Related TGF-β Receptor TNF Receptor Parasite Inflammation/Immunology
    Skimmin (Umbelliferone glucoside) is a major pharmacologically active and orally active molecule present in Hydrangea paniculata, a medical herb used in traditional Chinese medicine as an anti-inflammatory agent. Skimmin has renal protective activity. Skimmin can improve creatinine clearance, and reduce plasma creatinine, and kidney injuries. Skimmin has good anti-amoebic activity against the HM1:IMMS strain of Entamoeba histolytica. Skimmin has anti-cancer and neuroprotective activities. Skimmin reduces cardiac fibrosis as well as decreasing TNF-α, IL-6, IL1β, and TGFβ1 in cardiac tissues. Skimmin can be studied in research for diabetes and diabetes-related diseases .
    Skimmin

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