Vosilasarm
Based on 6 publication(s) in Google Scholar
Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors.
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- Purity: 99.80%
- CAS No.: 1182367-47-0
- 화학식: C20H16ClN5O2
- 분자량:393.83
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vosilasarm
More- J Biol Chem. 2024 Sep 12:107765. [Abstract]
- Metabolites. 2021 Feb 1;11(2):85. [Abstract]
- Drug Test Anal. 2022 Feb;14(2):349-370. [Abstract]
- Drug Test Anal. 2021 May;13(5):916-928. [Abstract]
- Drug Test Anal. 2021 Feb;13(2):283-298. [Abstract]
- J Steroid Biochem Mol Biol. 2019 May:189:81-86. [Abstract]
Biological Activity
Ki: 7 nM (Androgen receptor)[1]
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Cell Line
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Type | Value | Description | References |
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| C2C12 | EC50 |
0.1 nM
Compound: 7, RAD140
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Agonist activity at androgen receptor expressed in mouse C2C12 cells assessed as osteoblast differentiation after 5 days
Agonist activity at androgen receptor expressed in mouse C2C12 cells assessed as osteoblast differentiation after 5 days
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[PMID: 24900290] |
Vosilasarm (0-300 nM; pretreated for 1 hour) increases neuron viability against Aβ in a concentration-dependent manner[2].
Vosilasarm (100 nM; 1 hour) protects cultured neurons against apoptotic insults. Vosilasarm shows protective profiles of significantly protecting against neuronal death induced by Aβ and AAII, but not H2O2[2].
Vosilasarm (100 nM; 15 minutes) induces a significant increase in levels of phosphorylated but not total ERK in neuronal cultures[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In castrated immature rats, Vosilasarm (0.03-0.3 mg/kg; for 11 days) stimulates the levator ani bulbocavernosus muscle weight and prostate weight[1].
A high dose of Vosilasarm (10 mg/kg, p.o.) actually antagonizes the effect of testosterone propionate (TP) at 1 mg/kg on the seminal vesicles but adds to the effect of TP on the levator ani muscle. The effective dose for achieving antagonism by Vosilasarm is 0.3-1 mg/kg (p.o.) for 1 mg/kg TP (s.c.). In the young castrate male rat model, Vosilasarm appears to be a potent and complete androgen agonist on the levator ani, but a weaker, partial antagonist on the seminal vesicle and possibly the prostate[1].
Vosilasarm is neuroprotective in vivo using the rat kainate lesion model. In experiments with gonadectomized, adult male rats, Vosilasarm is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1182367-47-0
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Appearance Solid
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분자량 393.83
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화학식 C20H16ClN5O2
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Color White to off-white
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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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Synonyms
RAD140; EP0062
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Sep 12:107765. PMID: 39276936 -
Metabolites
Investigation of Equine In Vivo and In Vitro Derived Metabolites of the Selective Androgen Receptor Modulator (SARM) ACP-105 for Improved Doping Control. [Abstract]2021 Feb 1;11(2):85. PMID: 33535528 -
Drug Test Anal
Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes. [Abstract]2022 Feb;14(2):349-370. PMID: 34714606 -
Drug Test Anal
An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile. [Abstract]2021 May;13(5):916-928. PMID: 33283964 -
Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861 -
J Steroid Biochem Mol Biol
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. [Abstract]2019 May:189:81-86. PMID: 30825507
용액&용해도
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.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Miller CP, et al. Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Med Chem Lett. 2010 Dec 2;2(2):124-129. [Content Brief]
[2]. Jayaraman A, et al. Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Endocrinology. 2014 Apr;155(4):1398-1406. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5392 mL | 12.6958 mL | 25.3917 mL | 63.4792 mL |
| 5 mM | 0.5078 mL | 2.5392 mL | 5.0783 mL | 12.6958 mL | |
| 10 mM | 0.2539 mL | 1.2696 mL | 2.5392 mL | 6.3479 mL | |
| 15 mM | 0.1693 mL | 0.8464 mL | 1.6928 mL | 4.2319 mL | |
| 20 mM | 0.1270 mL | 0.6348 mL | 1.2696 mL | 3.1740 mL | |
| 25 mM | 0.1016 mL | 0.5078 mL | 1.0157 mL | 2.5392 mL | |
| 30 mM | 0.0846 mL | 0.4232 mL | 0.8464 mL | 2.1160 mL | |
| 40 mM | 0.0635 mL | 0.3174 mL | 0.6348 mL | 1.5870 mL | |
| 50 mM | 0.0508 mL | 0.2539 mL | 0.5078 mL | 1.2696 mL | |
| 60 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0580 mL | |
| 80 mM | 0.0317 mL | 0.1587 mL | 0.3174 mL | 0.7935 mL | |
| 100 mM | 0.0254 mL | 0.1270 mL | 0.2539 mL | 0.6348 mL |
Vosilasarm Related Classifications
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