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low clearance

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12839
    p38 MAPK-IN-1
    Maximum Cited Publications
    8 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

    		CDK Cancer
    JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.
    JH-XVI-178
  • 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-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-163040
    DOTA-Tyr-Lys-DOTA

    		Others 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
    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-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

    		Glucosidase 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

    		Others 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-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-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-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

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