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Purity: ≥98%
Testolone (formerly known as RAD140) is a novel, potent, nonsteroidal, orally bioavailable selective androgen receptor modulator (SARM) that is being researched for the treatment of diseases like breast cancer and muscle atrophy. Both male rats with kainate lesions and cultured neurons show neuroprotective effects from RAD140. RAD140 was found to be equally efficacious as testosterone in mitigating apoptotic insult-induced cell death in cultured hippocampal neurons. It was demonstrated that ERK phosphorylation was elevated and that the MAPK kinase inhibitor U0126 inhibited protection, indicating that RAD140 neuroprotection was mechanistically dependent upon MAPK signaling. Importantly, employing the rat kainate lesion model, RAD140 was also neuroprotective in vivo.
| ln Vitro |
In a concentration-dependent manner, vosilasarm (0-300 nM; pretreated for 1 hour) increases neuron viability against Aβ[2].
In cultured neurons, vosilasarm (100 nM; 1 hour) guards against apoptotic insults. Vosilasarm exhibits protective profiles that considerably guard against Aβ and AAII-induced neuronal death, but not H2O2[2]. In neuronal cultures, votilasarm (100 nM; 15 minutes) significantly raises the levels of phosphorylated ERK, but not total ERK[2]. |
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| ln Vivo |
Vosilasarm exhibits good bioavailability in rats (F = 27-63%) and monkeys (65-75%), as well as high stability (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes[1].
Vosilasarm (0.03-0.3 mg/kg; for 11 days) increases the weight of the prostate and the levator ani bulbocavernosus muscle in immature castrated rats[1]. The effect of testosterone propionate (TP) at 1 mg/kg on seminal vesicles is actually countered by a high dose of Vosilasarm (10 mg/kg, p.o. ), but TP's effect on the levator ani muscle is enhanced. Vosilasarm can induce antagonism at an effective dose of 0.3–1 mg/kg (p.o.) for 1 mg/kg TP (s.c.). Vosilasarm appears to be a strong and complete androgen agonist on the levator ani, but a weaker, partial antagonist on the seminal vesicle and potentially the prostate in the young castrate male rat model[1]. Vosilasarm is shown to be neuroprotective in vivo in the rat kainate lesion model. Vosilasarm has been shown in studies involving gonadectomized adult male rats to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as evidenced by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate[2]. |
| References |
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| Additional Infomation |
RAD140 is an investigational selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and breast cancer.
Vosilasarm is an orally bioavailable, non-steroidal selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activities. Upon oral administration, vosilasarm acts as an agonist in select tissues, such as skeletal muscle and bone, where it binds to and activates androgen receptors (ARs). In the prostate and breasts, vosilasarm acts as an antagonist and blocks AR activation and AR-mediated cellular proliferation. Therefore, this agent may improve bone formation and muscle mass and strength, and may inhibit both the growth of the prostate in males and AR-dependent breast cancer cell proliferation. Compared to anabolic agents, SARMs have reduced androgenic properties. |
| Molecular Formula |
C20H16CLN5O2
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| Molecular Weight |
393.83
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| Exact Mass |
393.099
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| Elemental Analysis |
C, 61.00; H, 4.10; Cl, 9.00; N, 17.78; O, 8.12
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| CAS # |
1182367-47-0
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| Related CAS # |
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| PubChem CID |
44200882
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
687.7±65.0 °C at 760 mmHg
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| Flash Point |
369.7±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
3.02
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
623
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| Defined Atom Stereocenter Count |
2
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| 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
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| InChi Key |
XMBUPPIEVAFYHO-KPZWWZAWSA-N
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| InChi Code |
InChI=1S/C20H16ClN5O2/c1-11-16(8-7-15(10-23)17(11)21)24-18(12(2)27)20-26-25-19(28-20)14-5-3-13(9-22)4-6-14/h3-8,12,18,24,27H,1-2H3/t12-,18+/m0/s1
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| Chemical Name |
2-chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzonitrile
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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 (6.35 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 (6.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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: ≥ 2.5 mg/mL (6.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5392 mL | 12.6958 mL | 25.3917 mL | |
| 5 mM | 0.5078 mL | 2.5392 mL | 5.0783 mL | |
| 10 mM | 0.2539 mL | 1.2696 mL | 2.5392 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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Tissue-selective antagonist activity ofRAD140.ACS Med Chem Lett.2010 Dec 2;2(2):124-9. |
Tissue-selective agonist activity ofRAD140in young intact male rats.ACS Med Chem Lett.2010 Dec 2;2(2):124-9. |
Primate body weight from day −21, through 28 days dosing and 21 days postdosing withRAD140(0.01, 0.1, and 1 mg/kg, po).ACS Med Chem Lett.2010 Dec 2;2(2):124-9. |
RAD140 is neuroprotective against apoptotic insults.Endocrinology.2014 Apr;155(4):1398-406. |
RAD140 induces tissue-specific androgenic effects.Endocrinology.2014 Apr;155(4):1398-406. |
Quantitative analyses of MAPK signaling in SARM neuroprotection.Endocrinology.2014 Apr;155(4):1398-406. |
RAD140 reduces neuronal cell death cause by kainate.
RAD140 increases neuron viability against Aβ in a concentration-dependent manner.Endocrinology.2014 Apr;155(4):1398-406. |
Kainate-induced seizures are not affected by androgen status Behavioral features of kainate-induced seizures were monitored and quantified for a 3-hour period following the lesion.Endocrinology.2014 Apr;155(4):1398-406. |
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