| Size | Price | Stock | Qty |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
Andarine (formerly known as GTx-007; S-4; GTx007; S4) is an orally bioactive and selective non-steroidal androgen receptor (AR) agonist, specifically a selective androgen receptor modulator (SARM), that has potential usefulness in muscle wasting and osteoporosis. It activates AR with a Ki of 4 nM and is tissue-selective for anabolic organs. Andarine is being investigated for treating conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects.
| Targets |
Androgen receptor (AR). Andarine (GTx-007) acts as an AR agonist. In an in vitro cotransfection system at 10 nM, it stimulated AR‑mediated reporter gene expression to 93% of that observed for 1 nM dihydrotestosterone (DHT). No individual Ki or EC50 value for S‑4 is reported in the paper; the Ki values for the S‑isomers of compounds 1‑4 ranged from 4 to 37 nM [1]
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| ln Vitro |
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| ln Vivo |
In the prostate and seminal vesicles, GTx-007 (S-4) is only a partial agonist, returning them to 33.8 and 28.2% of intact animals, respectively[2]. Wnt4 and Wnt7a uterine expression was markedly elevated by GTx-007[2].
In castrated immature male rats, Andarine (GTx-007) (S‑4) produced dose‑dependent stimulation of prostate, seminal vesicle, and levator ani muscle growth after 14 days of subcutaneous administration. |
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| Enzyme Assay |
Recombinant full‑length K‑Ras(G12C) fully labelled with 12 (or unlabelled control) at ~10 μM is incubated with 200 μM mant‑dGDP in the presence of 2.5 M EDTA for 1 h at room temperature. MgCl₂ is then added to a final concentration of 10 mM, and the protein is passed through a NAP‑5 column to remove free nucleotide. The purified protein (1 μM final) in reaction buffer (20 mM HEPES pH 7.5, 150 mM NaCl, 1 mM DTT, 1 mM MgCl₂) is added to a low‑volume black‑bottom plate. Fluorescence intensity (excitation 360 nm, emission 440 nm) is measured to obtain a baseline. Then 5 μL of EDTA solution containing serial dilutions of unlabelled GDP or GTP is added, and the mixture is equilibrated for 2 h at room temperature. Fluorescence is measured again, and IC₅₀ values are obtained by sigmoidal curve fitting. [1]
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| Cell Assay |
Apoptosis assay (Annexin V‑FITC):
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| Animal Protocol |
Animal/Disease Models: Female C57BL/6J mice[2].
Doses: 0.5 mg/mouse. Route of Administration: Seven daily subcutaneous (sc) injections. Experimental Results: Resulted in a highly heterogeneous pattern of AR expression in all compartments, with a significant increase of AR-positive cells in the luminal epithelium compared to VC. Had approximately ten glands per uterine cross-section within an endometrium, with a compact stroma, consistent with overall endogenous steroid depletion. Did not detect any impact of GTx-007 on body weight. Male Sprague‑Dawley rats (90–100 g) were randomly distributed into groups (n=5 per group). One day before drug treatment, animals were surgically castrated. After 24 h of recovery, Alzet osmotic pumps (model 2002) prefilled with drug solutions were implanted subcutaneously in the scapular region. For Andarine (GTx-007), the drug was first dissolved in a minimal amount of ethanol and then diluted to final concentrations with PEG 300 (designated vehicle 1). Dose rates administered were 0.15, 0.35, 0.55, 0.75, and 1.05 mg/day (as per Table 1). Treatment lasted 14 days. At the end of the study, rats were weighed, anesthetized, and sacrificed. Blood was collected by abdominal aorta venipuncture. Ventral prostates, seminal vesicles, levator ani muscle, liver, kidneys, spleen, lungs, and heart were removed, cleared of extraneous tissue, weighed, and fixed in 10% neutral buffered formalin. Osmotic pumps were removed to verify correct operation [1]. |
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| Toxicity/Toxicokinetics |
Andarine (GTx-007) did not cause any drug‑ or dose‑related changes in total body weight or the weights of non‑reproductive organs (liver, heart, kidney, spleen, lungs). Complete diagnostic hematology studies (complete blood count and serum chemistry profiles, including AST, ALT, cholesterol, HDL, triglyceride) revealed no drug‑ or dose‑related abnormalities; all values remained within normal ranges. No signs of acute toxicity were observed during the 14‑day treatment period. Specifically, no hepatotoxicity or significant changes in serum lipids were noted [1].
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| References | ||
| Additional Infomation |
(2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propionamide is an aniline compound, belonging to the acetamide class. Andalin is a nonsteroidal selective androgen receptor modulator.
Andarine (GTx-007) (S‑4) is one of the first nonsteroidal SARMs with in vivo functional activity and tissue‑selective anabolic effects. Its mechanism of tissue selectivity may be due to differential cofactor recruitment or distinct in vivo disposition compared to steroidal androgens. Unlike testosterone, S‑4 is not amplified by 5α‑reductase in reproductive tissues, thus exhibiting reduced androgenic activity on prostate and seminal vesicles while maintaining potent anabolic activity on muscle. The compound did not suppress LH or FSH at therapeutically relevant doses (near ED₅₀ for anabolic effect), suggesting a reduced risk of feedback‑mediated hypogonadism. These properties make S‑4 a candidate for treating muscle‑wasting diseases, sarcopenia, and other conditions where anabolic effects are desired without androgenic side effects. The paper notes that further preclinical and clinical development is warranted [1]. |
| Molecular Formula |
C19H18F3N3O6
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| Molecular Weight |
441.36
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| Exact Mass |
441.114
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| CAS # |
401900-40-1
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| Related CAS # |
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| PubChem CID |
9824562
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
698.7±55.0 °C at 760 mmHg
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| Melting Point |
70-74ºC
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| Flash Point |
376.4±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
4.01
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
663
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)NC1=CC=C(C=C1)OC[C@@](C)(C(=O)NC2=CC(=C(C=C2)[N+](=O)[O-])C(F)(F)F)O
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| InChi Key |
YVXVTLGIDOACBJ-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C19H18F3N3O6/c1-11(26)23-12-3-6-14(7-4-12)31-10-18(2,28)17(27)24-13-5-8-16(25(29)30)15(9-13)19(20,21)22/h3-9,28H,10H2,1-2H3,(H,23,26)(H,24,27)/t18-/m0/s1
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| Chemical Name |
(2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5%Propylene glycol:30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2657 mL | 11.3286 mL | 22.6572 mL | |
| 5 mM | 0.4531 mL | 2.2657 mL | 4.5314 mL | |
| 10 mM | 0.2266 mL | 1.1329 mL | 2.2657 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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