S-40503
S-40503 is a tissue-selective androgen receptor (AR) agonist with a Ki of 14.9 nM for rat AR. S-40503 binds to AR with high specificity, exerts full agonistic effects in bone and muscle, acts as a partial agonist in the prostate, and preferentially targets anabolic tissues rather than androgen-dependent tissues. S-40503 can be used in the research of osteoporosis.
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- No. CAS: 404920-28-1
- Fòrmula: C15H23N3O3
- Peso molecular:293.36
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
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Rat AR 14.9 nM (Ki) |
In Vitro
S-40503 binds to androgen receptor with a relative binding affinity of 0.3% compared to DHT[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
S-40503 (30 mg/kg; s.c.; daily; 4 weeks) increases levator ani weight without enlarging the prostate in normal male rats, confirming diminished virilizing activity under physiological androgen conditions[1].
S-40503 (30 mg/kg; s.c.; daily; 8 weeks) stimulates periosteal bone formation to increase femoral cortical bone mass and biomechanical strength in ovariectomized rats, with no effect on cancellous bone[1].
S-40503 (30 mg/kg; s.c.; daily; 4 weeks) directly increases tibial cortical bone mass without affecting hindlimb muscle weight in immobilized orchiectomized rats, while maintaining muscle anabolic activity and reduced virilizing effects[1].
S-40503 (1-30 mg/kg; s.c.; daily; 4 weeks) acts as a tissue-selective androgen receptor agonist in castrated rats, showing similar anabolic activity in muscle and bone to DHT at the highest tested dose but with less stimulatory effect on prostate growth[2].
S-40503 (30 mg/kg; s.c.; daily; 4 weeks) exhibits tissue selectivity in intact male rats, stimulating anabolic muscle growth without affecting prostate tissue weight at the tested dose[2].
S-40503 (s.c.; daily) acts as an anabolic agent to restore bone density, formation, and strength in ovariectomized rats with established osteoporosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 11-week-old, 320 to 340 g, bilateral orchiectomy-induced hypogonadism)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:s.c.; daily; 4 weeks
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Result:Increased prostate weight dose-dependently starting at 10 mg/kg.
Reached ~75% of sham levels and plateaued at 30 mg/kg.
Increased levator ani weight significantly at 30 mg/kg, exceeding sham levels.
Increased femoral BMD significantly at 30 mg/kg, exceeding sham levels.
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Animal Model:Sprague-Dawley (male, 11-week-old, 320 to 340 g)[1]
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Dosage:30 mg/kg
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Administration:s.c.; daily; 4 weeks
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Result:Left prostate weight unchanged relative to vehicle-treated normal rats.
Increased levator ani weight significantly relative to vehicle-treated normal rats.
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Animal Model:Sprague-Dawley (female, 11-week-old, 200 to 230 g, bilateral ovariectomy-induced postmenopausal bone loss)[1]
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Dosage:30 mg/kg
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Administration:s.c.; daily; 8 weeks
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Result:Increased femoral cortical bone BMD significantly relative to vehicle-treated ovariectomized rats.
Elevated periosteal mineral apposition rate (MAR) markedly relative to vehicle-treated ovariectomized rats.
Increased maximum load and breaking energy of femoral cortical bone significantly relative to vehicle-treated ovariectomized rats, with stiffness showing a non-significant upward trend.
Left femoral cancellous bone BMD unchanged relative to vehicle-treated ovariectomized rats.
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Animal Model:Sprague-Dawley (male, 11-week-old, 320 to 340 g, bilateral orchiectomy combined with right hindlimb sciatic neurectomy/immobilization)[1]
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Dosage:30 mg/kg
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Administration:s.c.; daily; 4 weeks
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Result:Left gastrocnemius muscle weight unchanged relative to vehicle-treated orchiectomized/neurectomized rats.
Kept prostate weight similar to sham and neurectomy-only rats.
Increased levator ani weight significantly relative to vehicle-treated orchiectomized/neurectomized rats.
Increased tibial cortical bone BMD significantly relative to vehicle-treated orchiectomized/neurectomized rats.
Left tibial cancellous bone BMD unchanged relative to vehicle-treated orchiectomized/neurectomized rats.
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Animal Model:Male rats (strain not specified)[2]
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Dosage:1 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:s.c.; daily; 4 weeks
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Result:Increased prostate and levator ani muscle weights significantly at 10 and 30 mg/kg/day.
Increased femoral BMD statistically significantly only at 30 mg/kg/day.
Restored prostate weight to ~80% of intact control levels at 30 mg/kg/day.
Restored levator ani muscle weight to ~115% of intact control levels at 30 mg/kg/day.
Increased femoral BMD to a level similar to DHT at 10 mg/kg/day at 30 mg/kg/day.
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Animal Model:Male rats (strain not specified)[2]
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Dosage:30 mg/kg
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Administration:s.c.; daily; 4 weeks
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Result:Increased levator ani muscle weight by 30% at 30 mg/kg/day.
Did not significantly change prostate weight at 30 mg/kg/day.
Chemical Information
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No. CAS 404920-28-1
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Peso molecular 293.36
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Fòrmula C15H23N3O3
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SMILES
CC(CO)(C)C1CC(N(C)C)C2=CC([N+]([O-])=O)=CC=C2N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Ficha de datos (286 KB)
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SDS (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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