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low clearance

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32

Inhibitors & Agonists

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Screening Libraries

2

Biochemical Assay Reagents

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Oligonucleotides

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153241
    GSK737

    		Epigenetic Reader Domain Cancer
    GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
    GSK737
  • HY-12839
    p38 MAPK-IN-1
    Maximum Cited Publications
    12 Publications Verification

    		 p38 MAPK Autophagy Inflammation/Immunology
    p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
    p38 MAPK-IN-1
  • HY-139875
    JH-XVI-178
    1 Publications Verification

    		 CDK Cancer
    JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties .
    JH-XVI-178
  • 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-128060
    PDE5-IN-42

    		Phosphodiesterase (PDE) Cardiovascular Disease
    PDE5-IN-42 (Compound 42) is a potent and orally active PDE5 inhibitor with an IC50 of 0.04 nM. PDE5-IN-42 maintains selectivity over PDE6 and PDE11 .
    PDE5-IN-42
  • HY-173006
    AZ3246

    		MAP4K Interleukin Related Cancer
    AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound .
    AZ3246
  • HY-163040
    DOTA-Tyr-Lys-DOTA

    		Biochemical Assay Reagents Inflammation/Immunology
    DOTA-Tyr-Lys-DOTA is a DOTA-based small molecule hapten. DOTA-Tyr-Lys-DOTAexhibits rapid clearance and low whole-body retention. DOTA-Tyr-Lys-DOTA can used in study pretargeted radioimmunotherapy .
    DOTA-Tyr-Lys-DOTA
  • HY-120004
    PF-06827443

    		mAChR Infection
    PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
    PF-06827443
  • HY-112047
    GSK8175

    GSK2878175

    		 HCV Infection
    GSK8175 is a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV). GSK8175 is a sulfonamide- N-benzoxaborole analog with low in vivo clearance across preclinical species and broad-spectrum activity against HCV replicons .
    GSK8175
  • 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-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-176204
    Axl-IN-19

    		TAM Receptor Cancer
    Axl-IN-19 (Compound 68) is a selective AXL (a membrane-bound receptor tyrosine kinase) inhibitor (IC50: 5.3 nM; Cellular KD = 6.8 nM). Axl-IN-19 has favorable rat PK with low clearance and moderate bioavailability. Axl-IN-19 can be used for cancer research .
    Axl-IN-19
  • 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-153256
    EP3 antagonist 4

    		Prostaglandin Receptor Metabolic Disease
    EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .
    EP3 antagonist 4
  • HY-154823
    Gcase activator 2

    		Glycosidase Metabolic Disease
    Gcase activator 2 (compound 14), a pyrrolo[2,3-b]pyrazine, is alos a β-Glucocerebrosidase (GCase) activator (EC50=3.8 μM). Gcase activator 2 induces GCase dimerizatio (both K-type and V-type). And Gcase activator 2 has low metabolic clearance in human and mouse .
    Gcase activator 2
  • HY-143439
    LX-039

    		Estrogen Receptor/ERR Cancer
    LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
    LX-039
  • 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-150080
    GSK3739936

    BMS-986180

    		 HIV HIV Integrase Infection
    GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
    GSK3739936
  • HY-162238
    OSM-S-106

    		Parasite Infection
    OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
    OSM-S-106
  • HY-12570
    CK2-IN-9

    		Casein Kinase Wnt Cancer
    CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC50 of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC50 of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat .
    CK2-IN-9
  • HY-168957
    RuDiOBn

    		MMP Reactive Oxygen Species Others
    RuDiOBn scanvages DPPH and ABTS free radicals (13.2% and 5.9% clearance at 100 μg/mL), exhibits low antioxidant activity. RuDiOBn inhibits the collagen glycation, reduces the formation of advanced glycation end products (AGEs) with an IC50 of 2.45 μg/mL. RuDiOBn enhances the proliferation and migration of fibroblasts, stimulates the synthesis of collagen, promoting the skin repair and regeneration. RuDiOBn also inhibits collagenase .
    RuDiOBn
  • HY-122229
    GS-9822

    		HIV Infection
    GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
    GS-9822
  • HY-155518
    IRAK4-IN-25

    		IRAK Inflammation/Immunology
    IRAK4-IN-25 (compound 38) is an orally acitve and potent IRAK4 inhibitor (IC50=7.3 nM), with low clearance (Cl=12 mL/min/kg). IRAK4-IN-25 inhibits production of pro-inflammatory cytokines, and shows in vitro safety and ADME profiles. IRAK4-IN-25 can be used for research in inflammatory and autoimmune disorders .
    IRAK4-IN-25
  • HY-146113
    IRAK4-IN-15

    		IRAK Cancer
    IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .
    IRAK4-IN-15
  • HY-163476
    PIP5K1C-IN-1

    		PI4P5K Inflammation/Immunology Cancer
    PIP5K1C-IN-1 (Compound 30) is a potent PIP5K1C inhibitor, with an IC50 of 0.80 nM. PIP5K1C-IN-1 exhibits low total clearance in mice and high levels of kinase selectivity. PIP5K1C-IN-1 can be used for the research of cancer and chronic pain .
    PIP5K1C-IN-1
  • HY-136659
    Ro 04-5595

    		iGluR Others
    Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds .
    Ro 04-5595
  • HY-159091
    HIV-1 integrase inhibitor 12

    		HIV Integrase Infection
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
    HIV-1 integrase inhibitor 12
  • 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-172732
    PRMT5-IN-50

    		Histone Methyltransferase Cancer
    PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice .
    PRMT5-IN-50
  • HY-162585
    5-HT1AR agonist 1

    		5-HT Receptor Neurological Disease
    5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
    5-HT1AR agonist 1
  • HY-112624E
    Dextran T0.8 (MW 800)

    Dextran 0.8; Dextran D0.8; Dextran T0.8(MW 640-960)

    		 Biochemical Assay Reagents Others
    Dextran T0.8 (Dextran 0.8; Dextran T0.8(MW 640-960)) is a food additive with a porous network structure that exhibits strong hydration capacity and low browning activity. Dextran T0.8 (MW 800) can improve the coagulation of dairy products and is used as a prebiotic in baked goods. Dextran T0.8 (MW 800) is non-toxic to HeLa cells at a concentration of ~500 μg/mL and has a low relative browning rate in the Maillard reaction. The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong the half-life of drugs, increase local concentrations, and reduce the activity of immune clearance .
    Dextran T0.8 (MW 800)
  • HY-112624B
    Dextran T70 (MW 70,000)

    Dextran 70; Dextran D70; Dextran T70(MW 64000-76000)

    		 Bacterial Others
    Dextran 70,000 is a high molecular weight polysaccharide formed by glucose linked by α-(1→6) glycosidic bonds. Dextran 70,000 can expand blood volume through colloidal osmotic pressure effect and inhibit cell adhesion and platelet aggregation through steric hindrance. At the same time, Dextran 70,000 can be used as a drug carrier to achieve targeted delivery through endocytosis. Dextran 70,000 is biologically inert and has low immunogenicity. It can be used for clinical blood volume expansion, anti-thrombotic research, and evaluation of vascular permeability in in vitro experiments. It can also be combined with fluorescent dyes for cell tracking and drug delivery research. The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong the half-life of drugs, increase local concentrations, and reduce the activity of immune clearance.
    Dextran T70 (MW 70,000)

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