Identification | Back Directory | [Name]
Andarine | [CAS]
401900-40-1 | [Synonyms]
GTx007 GTx-007 MK-2866 sarM s4 Andarine Ostarine 401900-40-1 Andarine(S4) S-4(Andarine ) Andarine, >=99% Andarine,GTK-007 Andarine (GTX-007) Andarine,GTX-007/GTX007 OSTARINE(MK-2866),ENOBOSARM 3-(4-acetaMidophenoxy)-2-hydroxy-2-Methyl-N-[4-nitro-3-(trifluoroMethyl)phenyl]propanaMide (2R)-3-(4-Cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide (S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)phenyl)propanamide (2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide N-[4-Nitro-3-(trifluoromethyl)phenyl]-(2S)-3-[4-(acetylamino)phenoxy]-2-hydroxy-2-methylpropanamide Propanamide,3-[4-(acetylamino)phenoxy]-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phe nyl]-,(2S)- N-[4-Nitro-3-(trifluoromethyl)phenyl]-(2S)-3-[4-(acetylamino)phenoxy]-2-hydroxy-2-methylpropanamide Andarine | [Molecular Formula]
C19H18F3N3O6 | [MDL Number]
MFCD09027386 | [MOL File]
401900-40-1.mol | [Molecular Weight]
441.36 |
Questions And Answer | Back Directory | [Selective Androgen Receptor Modulator]
Andarine (MK-2866), as the arylpropionamide derivate, has been developed in pharmaceutical industry as a new class of therapeutics called Selective Androgen Receptor Modulator (SARM, either agonists or antagonists at particular androgen receptors) with specific selectivity for particular tissues and organs, that could substitute the synthetic anabolic drugs used in medical treatments.
| [Clinical Application]
The pharmacological activity of andarine suggest the great potential of andarine in the development of the clinically available SARMs, which offers unique therapeutic advantages over their steroidal counterparts and an exciting opportunity to differentially regulate the androgen effects in various target tissues, thus minimizing the interference to normal. Thus, andarine has promising in advanced clinical trials that aim to treat age-related maladies and to counteract symptoms of severe diseases such as sarcopenia and cancer cachexia.
However, andarine may be misused in sports where athletes and/or their handlers may seek to gain unfair advantage. Therefore, andarine as agonist is prohibited for use by the International Federation of Horseracing Authorities and the World Anti-Doping Agency.
| [Biological activity]
Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, and it is tissue selective for the metabolic organ. Phase 3. | [In vitro]
In vitro, Andarine binds to androgen receptors with high affinity with Ki of 4 nM. Moreover, 10 nM Andarine stimulated the transcription adjusted by androgen receptor, up to 93%. | [In vivo]
In vivo, Andarine has an effective metabolic activity, and stimulates the growth of the prostate, seminal vesicle, and levator ani, with ED50 is 0.43 mg/day, 0.55 mg/day, and 0.14 mg/day respectively. This effect is dose dependent. In addition, Andarine acts on FSH, which does not affect some physiological changes caused by castration, and at a dose of 0.5 mg or more per day, partially inhibiting LH production. Andarine was administered to dog intravenously at 0.1, 1, 3, and 10 mg/kg doses, then the total body clearance (CL) decreased from 7.4 mL/min/kg to 3.1 mL/min/kg, the steady-state volume (Vss) was 1.39 L/kg and the half-life was 229 minutes. In addition, Andarine was 10 mg/kg, 1 mg/kg and 0.1 mg/kg, with oral bioavailability of 38%, 62% and 91% respectively. Andarine has tissue selective pharmacological activity and is well treated with 0.5 mg/day concentration, significantly reducing prostate weight to 79.4%. | [Characteristics]
Andarine is a selective non-steroidal androgen receptor (AR) agonist. |
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