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Art. -Nr.: HY-103578

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S-40503

S-40503 is a tissue-selective androgen receptor (AR) agonist with a K_i 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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CAS. Nr.: 404920-28-1
Formel: C₁₅H₂₃N₃O₃
Molecular Weight:293.36

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (286 KB)

S-40503 Chemical Structure

CAS. Nr.: 404920-28-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]^[2]^[3]^[4]

Rat AR

14.9 nM (Ki)

In Vitro

S-40503 is a selective, high-affinity androgen receptor binder with minimal cross-reactivity to other nuclear receptors, exhibiting an AR K_i of 14.9 nM^[1].
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 (1-30 mg/kg; s.c.; daily; 4 weeks) exhibits potent anabolic activities on bone and muscle in orchiectomized rats, with prostate weight reaching ~75% of sham levels at the highest tested dose, demonstrating reduced virilizing activity relative to natural androgens^[1].
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.

Animal Model:

Sprague-Dawley (male, 11-week-old, 320 to 340 g, bilateral orchiectomy-induced hypogonadism)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

s.c.; daily; 4 weeks
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.

Animal Model:

Sprague-Dawley (male, 11-week-old, 320 to 340 g)^[1]
Dosage:

30 mg/kg
Administration:

s.c.; daily; 4 weeks
Result:

Left prostate weight unchanged relative to vehicle-treated normal rats.
Increased levator ani weight significantly relative to vehicle-treated normal rats.

Animal Model:

Sprague-Dawley (female, 11-week-old, 200 to 230 g, bilateral ovariectomy-induced postmenopausal bone loss)^[1]
Dosage:

30 mg/kg
Administration:

s.c.; daily; 8 weeks
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.

Animal Model:

Sprague-Dawley (male, 11-week-old, 320 to 340 g, bilateral orchiectomy combined with right hindlimb sciatic neurectomy/immobilization)^[1]
Dosage:

30 mg/kg
Administration:

s.c.; daily; 4 weeks
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.

Animal Model:

Male rats (strain not specified)^[2]
Dosage:

1 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

s.c.; daily; 4 weeks
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.

Animal Model:

Male rats (strain not specified)^[2]
Dosage:

30 mg/kg
Administration:

s.c.; daily; 4 weeks
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

CAS. Nr. 404920-28-1
Molecular Weight 293.36
Formel C₁₅H₂₃N₃O₃
SMILES

CC(CO)(C)C1CC(N(C)C)C2=CC([N+]([O-])=O)=CC=C2N1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hanada K, et al. Bone anabolic effects of S-40503, a novel nonsteroidal selective androgen receptor modulator (SARM), in rat models of osteoporosis. Biological & pharmaceutical bulletin. 2003 Nov;26(11):1563-9. [Content Brief]

[2]. Gao W, et al. Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands. Pharmaceutical research. 2006 Aug;23(8):1641-58.

[3]. Kearbey JD, et al. Effects of selective androgen receptor modulator (SARM) treatment in osteopenic female rats. Pharmaceutical research. 2009 Nov;26(11):2471-7.

[4]. Kearbey JD, et al. Selective Androgen Receptor Modulator (SARM) treatment prevents bone loss and reduces body fat in ovariectomized rats. Pharmaceutical research. 2007 Feb;24(2):328-35.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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