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MK-0773

CAS No. 606101-58-0

MK-0773( MK0773 | MK 0773 | PF 05314882 | PF-05314882 | PF05314882 )

Catalog No. M15267 CAS No. 606101-58-0

A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    MK-0773
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM.
  • Description
    A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM; displays no binding to other nuclear receptors ( GR, IC50> 2 uM) and 5α-reductase (IC50>10 uM); improves muscle function while minimizing effects on other tissues.Osteoporosis Phase 1 Clinical.
  • In Vitro
    The IC50 of MK-0773 binding to AR is increased 3.5-fold in the presence of 25% rat serum and 13-fold in the presence of 25% human serum, indicating that it binds to serum proteins. The affinity of MK-0773 for AR across species is evaluated using COS cells transfected with AR, and IC50 values are very similar in four species (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM).
  • In Vivo
    MK-0773 (6 and 80 mg/kg, s.c.) produces exposure-related stimulatory effects on cortical BFR and LBM in the OVX rat model. MK-0773 (5, 15, and 80 mg/kg, s.c.) increases seminal vesicle weights, and has reduced effects on the prostate. The partial agonism and tissue selectivity of MK-0773 does not translate into differential effects on lipid metabolism in OVX rats.
  • Synonyms
    MK0773 | MK 0773 | PF 05314882 | PF-05314882 | PF05314882
  • Pathway
    Endocrinology/Hormones
  • Target
    Androgen Receptor (AR)
  • Recptor
    Androgen Receptor (AR)
  • Research Area
    Metabolic Disease
  • Indication
    Osteoporosis

Chemical Information

  • CAS Number
    606101-58-0
  • Formula Weight
    479.5896
  • Molecular Formula
    C27H34FN5O2
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    C[C@@]12[C@@H](C(NCC3=NC4=CC=CN=C4N3)=O)CC[C@@]1([H])[C@]5([H])CC[C@@]6([H])N(C)C(C(F)=C[C@]6(C)[C@@]5([H])CC2)=O
  • Chemical Name
    1H-Indeno[5,4-f]quinoline-7-carboxamide, 3-fluoro-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-N-(3H-imidazo[4,5-b]pyridin-2-ylmethyl)-1,4a,6a-trimethyl-2-oxo-, (4aS,4bS,6aS,7S,9aS,9bS,11aR)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Schmidt A, et al. J Biol Chem. 2010 May 28;285(22):17054-64. 2. Papanicolaou DA, et al. J Nutr Health Aging. 2013;17(6):533-43.
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