| Field | Specification |
|---|---|
| Alternative names | RAD140; EP0062 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H16ClN5O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Vosilasarm, also known as RAD140 or EP0062, is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. It shows good selectivity over other steroid hormone nuclear receptors[1]. It is supplied as a white to off-white solid (C20H16ClN5O2, MW 393.83) at 99.46% purity.
Physical & Chemical Properties
| CAS Number | 1182367-47-0 |
|---|---|
| Molecular Formula | C20H16ClN5O2 |
| Molecular Weight | 393.83 g/mol |
| Purity | 99.46% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | ClC1=C(C)C(N[C@]([H])([C@@]([H])(O)C)C2=NN=C(O2)C3=CC=C(C#N)C=C3)=CC=C1C#N |
| Signaling Pathway | Vitamin D Related/Nuclear Receptor |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (253.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
Ki: 7 nM (Androgen receptor)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (253.92 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (6.35 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (6.35 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.35 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Pretreatment with Vosilasarm (0-300 nM; 1 hour) improves neuron viability against Aβ, with the effect scaling with concentration[2]. Cultured neurons are protected from apoptotic insults by Vosilasarm (100 nM; 1 hour). Its protection is significant against neuronal death induced by Aβ and AAII, but not against that induced by H2O2[2]. In neuronal cultures, Vosilasarm (100 nM; 15 minutes) significantly raises levels of phosphorylated ERK, but not total ERK[2].
In Vivo
Vosilasarm is highly stable with rat, monkey, and human microsomes (t1/2 > 2 h), and bioavailability is also good in rats (F = 27-63%) and in monkeys (65-75%)[1]. Treating castrated immature rats with Vosilasarm (0.03-0.3 mg/kg; for 11 days) increases the weight of the levator ani bulbocavernosus muscle and of the prostate[1]. At a high dose (10 mg/kg, p.o.), Vosilasarm in fact antagonizes the seminal vesicle effect of testosterone propionate (TP) at 1 mg/kg, yet adds to the TP effect on the levator ani muscle. The effective dose for Vosilasarm antagonism is 0.3-1 mg/kg (p.o.) against 1 mg/kg TP (s.c.). Using young castrate male rats, Vosilasarm appears to act as a potent and complete androgen agonist on the levator ani, and as a weaker, partial antagonist on the seminal vesicle and possibly on the prostate[1]. Neuroprotection by Vosilasarm is seen in vivo in the rat kainate lesion model. In gonadectomized adult male rats, Vosilasarm exhibits peripheral tissue-specific androgen action that largely spares the prostate, neural efficacy demonstrated through activation of androgenic gene regulation effects, and protection of hippocampal neurons from cell death after systemic administration of the excitotoxin kainate[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Investigation of Equine In Vivo and In Vitro Derived Metabolites of the Selective Androgen Receptor Modulator (SARM) ACP-105 for Improved Doping Control. Metabolites 2021 Feb 1;11(2):85. PMID: 33535528
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. J Biol Chem 2024 Oct;300(10):107765. PMID: 39276936
Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay. J Steroid Biochem Mol Biol 2019 May:189:81-86. PMID: 30825507
Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes. Drug Test Anal 2022 Feb;14(2):349-370. PMID: 34714606
An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile. Drug Test Anal 2021 May;13(5):916-928. PMID: 33283964
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. Drug Test Anal 2021 Feb;13(2):283-298. PMID: 32852861
