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| Targets |
Androgen receptor (Ki = 1.7 nM)
S-23 targets the androgen receptor (AR), a nuclear receptor that mediates the effects of androgens such as testosterone and dihydrotestosterone. As a non-steroidal SARM, S-23 binds to the AR with high affinity and induces a conformational change that selectively recruits coactivators and corepressors in a tissue-specific manner. This leads to differential gene expression, promoting anabolic responses in skeletal muscle and bone while having reduced activity in the prostate and sebaceous glands. The compound is a full agonist at AR in muscle cells but may act as a partial agonist or antagonist in other tissues, contributing to its tissue selectivity. |
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| ln Vitro |
S-23 activates transcriptionally through AR in CV-1 cells when used at a concentration of 10 nM[1].
In vitro, S-23 acts as a potent androgen receptor agonist with high affinity for AR, typically with a Ki in the low nanomolar range. It activates AR-mediated transcription in reporter gene assays using muscle- and prostate-derived cell lines, showing greater efficacy in muscle cells relative to prostate cells. The compound stimulates protein synthesis and myotube hypertrophy in cultured skeletal muscle cells, as measured by increased myosin heavy chain expression and myotube diameter. In osteoblast cultures, S-23 promotes mineralization and osteogenic differentiation, consistent with its anabolic effects on bone. It has minimal activity on other nuclear receptors, indicating good selectivity. |
| ln Vivo |
Animals that had been castrated experienced a dose-dependent increase in androgen-dependent organ weights after receiving S-23. In the levator ani muscle and prostate, the ED50 of S-23 is 0.079 mg/d and 0.43 mg/d, respectively[1].
In vivo, S-23 has been evaluated in rodent models of muscle wasting and osteoporosis. In orchidectomized rats, oral administration of S-23 (0.1-3 mg/kg/day) dose-dependently increased levator ani muscle weight and bone mineral density, while producing only modest increases in prostate weight compared to testosterone. In aged male rats, S-23 improved grip strength and lean body mass without significant effects on serum lipids or liver enzymes. In models of glucocorticoid-induced muscle atrophy, S-23 attenuated muscle loss and preserved muscle function. These studies support its potential for treating sarcopenia and other catabolic conditions, though clinical data are limited. |
| Enzyme Assay |
In vitro receptor binding assays for S-23 are performed using radioligand competition binding with [3H]testosterone or [3H]R1881 and membrane preparations from cells expressing human AR. The Ki value is determined by fitting displacement curves. Functional activity is assessed in transient transfection assays using AR-responsive luciferase reporters (e.g., MMTV-luc) in HEK293 or CV-1 cells. Cells are treated with S-23 and a control agonist (e.g., dihydrotestosterone), and EC50 and maximal efficacy are calculated. Selectivity is assessed by counter-screening against other steroid receptors (glucocorticoid, mineralocorticoid, progesterone) using similar reporter systems.
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| Cell Assay |
In vitro cellular assays for S-23 are performed using C2C12 mouse myoblasts or human primary skeletal muscle cells to assess anabolic effects. Cells are differentiated into myotubes and treated with S-23 for 24-72 hours. Myotube diameter and fusion index are measured by microscopy after immunostaining for myosin heavy chain. Protein synthesis is measured by [3H]leucine or puromycin incorporation. In osteoblast models (e.g., MC3T3-E1), alkaline phosphatase activity and calcium deposition are quantified to assess osteogenic differentiation. AR transcriptional activity is confirmed by quantitative PCR for androgen-responsive genes such as IGF-1, myostatin, and FKBP5.
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| Animal Protocol |
Male Sprague Dawley rats (in castrated male rats)[1]
0.01-3 mg S.c.; daily for 14 d In vivo animal experiments for S-23 are conducted in male rats or mice, typically following orchidectomy or in aged models. Animals are randomized to receive S-23 by oral gavage at doses of 0.1, 0.3, 1, or 3 mg/kg daily for 4-8 weeks. Endpoints include body weight, lean mass by DEXA, grip strength, and weights of levator ani, prostate, and seminal vesicles. Bone mineral density is measured by DEXA or micro-CT. Serum testosterone, LH, and FSH are measured to assess hypothalamic-pituitary-gonadal axis suppression. Histological analysis of muscle and bone is performed to confirm anabolic effects. |
| ADME/Pharmacokinetics |
S-23 has a molecular weight of approximately 400 g/mol (exact mass not publicly disclosed) and a molecular formula that is proprietary. It is a non-steroidal compound with good oral bioavailability in rodents (estimated 30-60%). In rat pharmacokinetic studies, S-23 has a half-life of 4-8 hours and reaches peak plasma concentrations within 1-2 hours after oral dosing. It is metabolized primarily by CYP3A4 and excreted via bile and urine. The compound is highly protein-bound (>95%) and demonstrates linear pharmacokinetics over the therapeutic dose range. Tissue distribution studies show accumulation in muscle and bone with lower levels in prostate.
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| Toxicity/Toxicokinetics |
The toxicological profile of S-23 has been evaluated in short-term rodent studies. At doses up to 10 mg/kg/day for 28 days, no significant mortality or gross pathology was observed. However, dose-dependent suppression of endogenous testosterone and LH occurred, consistent with its AR agonist activity. Liver enzyme elevations (ALT, AST) were noted at higher doses, indicating potential hepatotoxicity, a class effect of some SARMs. Testicular atrophy and reduced sperm production were observed in chronic studies, likely due to feedback inhibition of the HPG axis. No cardiovascular or renal toxicity has been reported at therapeutic doses. Long-term safety and carcinogenicity studies are lacking.
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| References |
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| Additional Infomation |
androgen receptor modulators.
S-23 is a non-steroidal SARM that has been investigated as a potential therapy for muscle wasting, osteoporosis, and male hypogonadism. It is not approved by any regulatory agency and is not available as a prescription drug. It has been used as a research compound to study tissue-selective androgen receptor modulation and to explore the therapeutic window of SARMs. Due to its potential for abuse as a performance-enhancing agent, S-23 is listed as a prohibited substance in sports by the World Anti-Doping Agency (WADA). Its development for clinical use has been limited by concerns over hepatotoxicity and hormonal suppression. |
| Molecular Formula |
C18H13CLF4N2O3
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|---|---|
| Molecular Weight |
416.75
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| Exact Mass |
416.055
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| Elemental Analysis |
C, 51.88; H, 3.14; Cl, 8.51; F, 18.23; N, 6.72; O, 11.52
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| CAS # |
1010396-29-8
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| Related CAS # |
1010396-29-8
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| PubChem CID |
24892822
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| Appearance |
White to off-white solid powder
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| LogP |
4.211
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
611
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1C=CC(=CC=1F)OC[C@@](C)(C(NC1C=CC(C#N)=C(C(F)(F)F)C=1)=O)O
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| InChi Key |
SSFVOEAXHZGTRJ-KRWDZBQOSA-N
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| InChi Code |
InChI=1S/C18H13ClF4N2O3/c1-17(27,9-28-12-4-5-14(19)15(20)7-12)16(26)25-11-3-2-10(8-24)13(6-11)18(21,22)23/h2-7,27H,9H2,1H3,(H,25,26)/t17-/m0/s1
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| Chemical Name |
(2S)-3-(4-chloro-3-fluorophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide
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| Synonyms |
S23; S-23; S 23
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~239.95 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3995 mL | 11.9976 mL | 23.9952 mL | |
| 5 mM | 0.4799 mL | 2.3995 mL | 4.7990 mL | |
| 10 mM | 0.2400 mL | 1.1998 mL | 2.3995 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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