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 제품안내  맞춤 서비스   Drug Discovery Service

Drug Candidate Assessment Package (Drug 후보물질 평가 팩키지)

Drug 후보물질의 characterization을 돕는 평가 팩키지를 추천해 드립니다.

Eurofins
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특징
  • Drug 후보물질의 characterization을 돕는 평가 팩키지를 추천해 드립니다.
  CORE PACKAGE BIOAVAILABILITY
  Bioavailability
  Ref. Assay name
  G228 Aqueous solubility (PBS, SGF, SIF) (1)
  2194 Protein binding (plasma, human) (2)
  3318 A-B permeability (Caco-2, pH 6.5/7.4)
  3320 B-A permeability (Caco-2, pH 6.5/7.4)
  0607 Intrinsic clearance (liver microsomes, human) (2)
     
     
  CORE PACKAGE DRUG INTERACTIONS
  CYP INHIBITION
  Ref. Assay name
  G232 CYP INHIBITION
  2064 CYP1A inhibition (HLM (3), phenacetin substrate)
  2065 CYP2B6 inhibition (HLM, bupropion substrate)
  2244 CYP2C8 inhibition (HLM, paclitaxel substrate)
  2066 CYP2C9 inhibition (HLM, diclofenac substrate)
  1772 CYP2C19 inhibition (HLM, omeprazole substrate)
  1838 CYP2D6 inhibition (HLM, dextromethorphan substrate)
  1770 CYP3A inhibition (HLM, midazolam substrate)
  1769 CYP3A inhibition (HLM, testosterone substrate)
  DRUG TRANSPORTERS
  Ref. Assay name
  1324 P-gp inhibition (MDR1-MDCKII, calcein AM substrate) (4)
  3633 BCRP inhibition (BCRP-CHO, Hoechst 33342 substrate) (4)
  3878 MRP1 inhibition (MRP1-HEK, calcein AM substrate)
  3879 MRP2 inhibition (MRP2-HEK, CDCF substrate)
  3880 MRP3 inhibition (MRP3-HEK, CDCF substrate)
  3658 OAT1 inhibition (OAT1-CHO, CF substrate) (4)
  3659 OAT3 inhibition (OAT3-CHO, CF substrate) (4)
  3660 OATP1B1 inhibition (OATP1B1-CHO, FMTX substrate) (4)
  3661 OATP1B3 inhibition (OATP1B3-CHO, FMTX substrate) (4)
  3746 OCT1 inhibition (OCT1-CHO, ASP+ substrate) (5)
  3726 OCT2 inhibition (OCT2-CHO, ASP+ substrate) (4)
  3656 ASBT inhibition (ASBT-CHO, 3H-taurocholic acid substrate)
  3657 NTCP inhibition (NTCP-CHO, 3H-taurocholic acid substrate)
  CYP INDUCTION
  Ref. Assay name
  3860 CYP1A2 induction (human hepatocytes, mRNA level, 3 donors)
  3861 CYP2B6 induction (human hepatocytes, mRNA level, 3 donors)
  3864 CYP3A4 induction (human hepatocytes, mRNA level, 3 donors)
     
     
  CORE PACKAGE IN VITRO TOXICITY
  CYTOTOXICITY
  Ref.  Assay name
  G202  Cytotoxicity (HepG2, 5 endpoints, HCA)
  CARDIAC TOXICITY
  Ref. Assay name
  2245 hERG (automated patch-clamp)
  2393 Nav1.5 (automated patch-clamp)
  GENOTOXICITY
  Ref. Assay name
  G175  Ames fluctuation test (TA98, TA100, TA1535, TA1537; with and without S9)
  1560 In vitro micronucleus (CHO-K1, without S9)
  1684 In vitro micronucleus (CHO-K1, with S9)
     
  (1) PBS = Phosphate Buffered Saline;SGF = Simulated Gastric Fluid;SIF = Simulated Intestinal Fluid
  (2) Additional Species Available
  (3) HLM = Human Liver Microsomes
  (4) recommended by FDA and EMA
  (5) recommended by EMA

 

  CORE PACKAGE SAFETY SCREEN 44
  Family  Ref.  Assay name
  RECEPTORS    
  Adenosine  0004 A2A (agonist radioligand)
  Adrenergic  2338 a1A (antagonist radioligand)
    0013  a2A (antagonist radioligand)
    0020  b2 (agonist radioligand)
    0018  b1 (agonist radioligand)
  Cannabinoid  0036  CB1 (agonist radioligand)
    0037  CB2 (agonist radioligand)
  Cholecystokinin  0039  CCK1 (CCKA) (agonist radioligand)
  Dopamine  0044  D1 (antagonist radioligand)
    1322  D2S (agonist radioligand)
  Endothelin  0054  ETA (agonist radioligand)
  Histamine  0870  H1 (antagonist radioligand)
    1208 H2 (antagonist radioligand)
  Muscarinic  0091  M1 (antagonist radioligand)
    0093  M2 (antagonist radioligand)
    0095  M3 (antagonist radioligand)
  Opioid and opioid-like  0114  delta2 (DOP) (agonist radioligand)
    1971 kappa (KOP) (agonist radioligand)
    0118  mu (MOP) (agonist radioligand)
  Serotonin  0131  5-HT1A (agonist radioligand)
    0132  5-HT1B (antagonist radioligand)
    0471  5-HT2A (agonist radioligand)
    1333 5-HT2B (agonist radioligand)
  Vasopressin  0159  V1a (agonist radioligand)
  Steroid nuclear receptors  0933  AR (agonist radioligand)
    0469  GR (agonist radioligand)
  Other receptors  3029 N neuronal a4b2 (agonist radioligand)
  ION CHANNELS    
  Voltage-gated channels  0161  Ca2+- L (dihydropyridine site)
    1868 hERG (membrane preparation)
    0166 KV
    0169 Na+- site 2
  Membrane ligand-gated channels  0028  BZD (central)
    0066  NMDA
    0411  5-HT3
  TRANSPORTERS    
  Dopamine  0052  dopamine transporter
  Norepinephrine  0355  norepinephrine transporter
  Serotonin  0439  5-HT transporter
  KINASES    
  Protein-tyrosine kinases  2906 Lck kinase
  OTHER ENZYMES    
  Phosphodiesterases  2432 PDE3A
    2434 PDE4D2
  Monoamine & neurotransmitter synthesis & metabolism
    0363  acetylcholinesterase
    0443  MAO-A (antagonist radioligand)
  Arachidonic acid metabolism  0726  COX1
    0727  COX2
       
  FOLLOW-UP 
  P-gp substrate assessment (Caco-2)
  Ref. Assay name
  3319 A-B permeability (Caco-2, pH 7.4/7.4)
  3321 B-A permeability (Caco-2, pH 7.4/7.4)
  3325 A-B permeability (Caco-2, pH 7.4/7.4 + verapamil)
  3326 B-A permeability (Caco-2, pH 7.4/7.4 + verapamil)
  CYP-Phenotyping
  Ref. Assay name
  1645 Intrinsic clearance (CYP1A2)
  2387 Intrinsic clearance (CYP2B6)
  2384 Intrinsic clearance (CYP2C8)
  1646 Intrinsic clearance (CYP2C9)
  1647 Intrinsic clearance (CYP2C19)
  1648 Intrinsic clearance (CYP2D6)
  1649 Intrinsic clearance (CYP3A4)
  Time-Dependent CYP Inhibition (HLM, package of 10 assays)
  Ref. Assay name
  G197 Time-dependent CYP1A inhibition (HLM, phenacetin substrate ± NADPH)
  G199 Time-dependent CYP2C9 inhibition (HLM, diclofenac substrate ± NADPH)
  G198 Time-dependent CYP2C19 inhibition (HLM, omeprazole substrate ± NADPH)
  G200 Time-dependent CYP2D6 inhibition (HLM, dextromethorphan substrate ± NADPH)
  G201 Time-dependent CYP3A inhibition (HLM, midazolam substrate ± NADPH)