Pharmacelsus

In vitro & in vivo Pharmacology Services

To gain profound and relevant preclinical data on efficacy and potency, in-depth knowledge of the corresponding disease is a key success factor. Pharmacelsus has a proven track record on conducting in vitro and in vivo studies on potency, selectivity and efficacy in several indication areas.

In vitro pharmocology assays

5α Reductase Inhibitors

  • Human recombinant isoenzymes type I und II

Aromatase Inhibitors

  • Recombinant human aromatase (CYP 19)

CYP17 Inhibitors

  • Human recombinant CYP 17

LHRH-A(nta)gonists

  • Interaction with LHRH-induced LH secretion in primary rat pituitary cells
Gluco- and Mineralo-corticoid Biosynthesis Inhibitors
  • Human steroid-secreting adrenocortical cell line

Inflammation

  • Cytokine induction (PMBC, monocytes), Luminex
  • Histamine release (mastocytes)

Assay Development and Implementation

  • Literature search
  • Validation with reference compounds
  • Implementation

In vivo pharmocology models

Model Development and Implementation

  • Literature search
  • Application to animal welfare authorities
  • Validation with reference compounds
  • Implementation

Diabetes / Metabolic Syndrome Models

  • Induced Models:
    • STZ Mice/Rats
    • DIO Mice/Rat
  • Genetic Models:
    • ob/ob Mice
    • db/db Mice
    • Zucker/ZDF Rat

Fibrosis Models

  • Liver Fibrosis:
    • Bile duct ligation in rats
    • Thioacetamide-induced liver fibrosis in rats
  • Kidney Fibrosis:
    • Unilateral ureter ligation in mice or rats

Cancer

  • In vivo model
    (immunodeficient mice)
  • Principle:
    s.c. tumor xenograft model
  • General Readouts:
    Tumor incidence, tumor size, tumor growth inhibition, terminal tumor weight, Occurence of metastases (postmortal)

Non-alcoholic Fatty Liver Disease

  • In vivo model
    (rat or mouse)
  • Principle:
    NAFLD induced by specific diets (high fat, high cholesterol)
  • General Readouts:
    Liver weight, clinical chemistry (e.g. ALT, AST, T-BIL, LDL, cholesterol etc.) in plasma, metabolic profile in plasma and tissue
  • Specific Readouts:
    Diabetic status, insulin resistance, triglycerides, LDL, inflammatory cytokines
  • Application:
    Proof of anti-steatotic effects

Steroid Endocrinology

  • 5a Reductase, Androgen Receptor:
    Readout: (anti-) androgenic activity as indicated by effects on prostate growth in castrated juvenile or adult rats
  • Aromatase, Estrogen Receptor:
    Readout: (anti-) estrogenic activity as indicated by effects on uterine growth in juvenile rats or ovariectomised adult rats

Steroid Endocrinology

  • LHRH-Receptor:
    Readout: LH levels in castrated rats
  • Aldosterone Synthase:
    Readout: aldosterone levels in ACTH-stimulated rats
  • CYP17 (17a-hydroxylase/ 17,20 lyase/ 17,20 desmolase):
    Readout: testosterone levels in adult rats

Leveraging our experience allows us to design, set-up and perform in vitro and in vivo pharmacology studies according to the specific requirements of your project.

Please contact us for your specific pharmacology study!

Dr. Ursula Mueller-Vieira
Head of ADMET & in vitro Pharmacology
mueller@pharmacelsus.de

Dr. Bettina Husen
Head of in vivo Pharmacology & Pharmacokinetics
husen@pharmacelsus.de