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Results for "

HLM

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16667
    HLM006474
    5 Publications Verification

    		 Early 2 Factor (E2F) Cancer
    HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
    HLM006474
  • HY-151540
    MMP-7-IN-1

    		MMP Cancer
    MMP-7-IN-1 is a potent and selective inhibitor of MMP-7 over MMP-1, -2, -3, -8, -9, -13 with an IC50 value of 10 nM. MMP-7 is a potential target for diseases including cancer and fibrosis .
    MMP-7-IN-1
  • HY-B2015
    Carbosulfan

    		Cytochrome P450 Parasite Infection
    Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers).
    Carbosulfan
  • HY-17614
    Ezutromid

    SMT C1100; BMN 195; VOX-C1100

    		 Cytochrome P450 Others
    Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
    Ezutromid
  • HY-N1483
    Guanfu base A

    		Potassium Channel Cardiovascular Disease
    Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
    Guanfu base A
  • HY-118339
    PF-4479745

    		5-HT Receptor Cancer
    PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension .
    PF-4479745
  • HY-146111
    IRAK4-IN-13

    		IRAK Cancer
    IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg .
    IRAK4-IN-13
  • HY-B2015S
    Carbosulfan-d18

    		Cytochrome P450 Parasite Infection
    Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
    Carbosulfan-d18
  • HY-153970
    URAT1 inhibitor 7

    		URAT1 Inflammation/Immunology
    URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research .
    URAT1 inhibitor 7
  • HY-155141
    hCYP3A4-IN-1

    		Cytochrome P450 Cancer
    hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
    hCYP3A4-IN-1
  • HY-135541
    Darexaban maleate

    YM150 maleate

    		 Others Cardiovascular Disease
    Darexaban maleate (YM150 maleate) is a direct factor Xa inhibitor with activity in preventing venous thromboembolism. The major metabolite of Darexaban maleate in humans is Darexaban glucitol, which acts pharmacologically. The glucitolation reaction of Darexaban maleate is mainly catalyzed by UGT1A9 and UGT1A10 in the human liver and intestine. The K(m) value of Darexaban maleate glucitolation in the liver is greater than 250 μM, while in the intestine it exhibits substrate inhibition kinetics with a K(m) value of 27.3 μM. The unbound K(m) value of Darexaban maleate is significantly reduced by the influence of fatty acid-free bovine serum albumin in both HLM and UGT1A9 .
    Darexaban maleate

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