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.

Physicochemical Properties

Molecular Formula	C19H18F3N3O6
Molecular Weight	441.36
Exact Mass	441.114
CAS #	401900-40-1
Related CAS #	401900-40-1
PubChem CID	9824562
Appearance	Light yellow to yellow solid powder
Density	1.5±0.1 g/cm3
Boiling Point	698.7±55.0 °C at 760 mmHg
Melting Point	70-74ºC
Flash Point	376.4±31.5 °C
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.605
LogP	4.01
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	6
Heavy Atom Count	31
Complexity	663
Defined Atom Stereocenter Count	1
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
InChi Key	YVXVTLGIDOACBJ-SFHVURJKSA-N
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
Chemical Name	(2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Synonyms	GTx-007;S-4;GTx007; S4;GTx 007; S 4
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	In vitro activity: Andarine stimulates AR-mediated transcription to 93% of that observed for 1 nM DHT at a concentration of 10 nM.
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].
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.
References	[1]. Pharmacodynamics of selective androgen receptor modulators. J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40. [2]. Selective androgen receptor modulators (SARMs) have specific impacts on the mouse uterus. J Endocrinol. 2019 Sep;242(3):227-239.
Additional Infomation	(2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide is an anilide and a member of acetamides. Andarine is a non-steroidal selective androgen receptor modulator.

Solubility Data

Solubility (In Vitro)

DMSO: 88 mg/mL (199.4 mM) Water:<1 mg/mL Ethanol:88 mg/mL (199.4 mM)

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. Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5%Propylene glycol:30mg/mL  (Please use freshly prepared in vivo formulations for optimal results.)

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.