A selective androgen receptor modulator
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MK-0773

Item No. 43202

Technical Information
Formal Name
(4aS,4bS,6aS,7S,9aS,9bS,11aR)-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-1H-indeno[5,4-f]quinoline-7-carboxamide
CAS Number
606101-58-0
Synonyms
  • PF-05314882
Molecular Formula
C27H34FN5O2
Formula Weight
Purity
≥90%
A solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@@]12[C@]3([H])[C@](CC[C@@]1([H])N(C(C(F)=C2)=O)C)([H])[C@@]4([H])[C@](CC3)([C@H](CC4)C(NCC5=NC6=NC=CC=C6N5)=O)C
InChi Code
InChI=1S/C27H34FN5O2/c1-26-11-10-17-15(6-9-21-27(17,2)13-19(28)25(35)33(21)3)16(26)7-8-18(26)24(34)30-14-22-31-20-5-4-12-29-23(20)32-22/h4-5,12-13,15-18,21H,6-11,14H2,1-3H3,(H,30,34)(H,29,31,32)/t15-,16-,17-,18+,21+,26-,27+/m0/s1
InChi Key
GBEUKTWTUSPHEE-JWJWXJQQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MK-0773 is a selective androgen receptor modulator (SARM).1 It selectively binds to the androgen receptor (AR; IC50 = 6.6 nM) over the glucocorticoid and progesterone receptors (IC50s = >2 µM for both). It is a partial agonist of AR that increases AR-dependent transcription in a reporter assay using MDA-MB-453 cells endogenously expressing AR. MK-0773 (6 mg/kg) increases the bone formation rate with less than a 5% increase in uterine weight in ovariectomized rats and increases seminal vesicle weight to a lesser extent than dihydrotestosterone (DHT) in orchidectomized rats when administered at a dose of 45 mg/kg. It reduces serum total cholesterol levels but also reduces serum HDL levels in ovariectomized rats when administered at a dose of 25 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schmidt, A., Kimmel, D.B., Bai, C., et alDiscovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology. The Journal of Biological Chemisty 285(22), 17054-17064 (2010).