Ostarine
目录号 : GC36820
Ostarine (GTx-024, MK-2866, Enobosarm) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
Cas No.:841205-47-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ostarine (GTx-024, MK-2866, Enobosarm) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
Ostarine at the concentration of 10 nM modulates the transcriptional activity of AR in CV-1 cells cotransfected with a human AR expression vector, a luciferase reporter vector, and a control β-galactosidase vector, with 94%-100% relative activity of the transcriptional activation observed for 1 nM DHT. [1] [2]
After intravenous administration of Ostarine at a single dose of 10 mg/kg, plasma concentration of Ostarine declines slowly, exhibiting a longer terminal half-life of 6.0 hours, as compared to that of other related cyano/nitro group-substituted SARMs with terminal halflives of 2.6-4.0 hours. Ostarine exhibits significantly androgenic and anabolic activity by stimulating the growth of prostate, seminal vesicles, and levator ani muscle when administered in castrated male rats; Ostarine is more potent than other cyano/nitro group-substituted SARMs. Ostarine restores the weight of the prostate to 39.2%, and seminal vesicle 78.8%, and stimulates the growth of levator ani muscle to a greater extent of 141.9% as compared with that of androgenic organs. Ostarine exhibits the highest in vivo androgenic and anabolic activity of any AR nonsteroidal agonist examined to date, with ED50 values of 0.12, 0.39 and 0.03 mg/day in prostate, seminal vesicles, and levator ani muscle, respectively, being 4 times as potent as testosterone propionate (TP) in levator ani muscle. At low dose of 0.03 mg/day, Ostarine is sufficient to exert efficacious and selective activity in anabolic tissues. [1]
[1] Kim J, et al. J Pharmacol Exp Ther, 2005, 315(1), 230-239. [2] Duke CB, et al. J Med Chem, 2011, 54(11), 3973-3976.
| Cas No. | 841205-47-8 | SDF | |
| Canonical SMILES | FC(F)(C1=CC(NC([C@](C)(COC2=CC=C(C=C2)C#N)O)=O)=CC=C1C#N)F | ||
| 分子式 | C19H14F3N3O3 | 分子量 | 389.33 |
| 溶解度 | DMSO: ≥ 100 mg/mL (256.85 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5685 mL | 12.8426 mL | 25.6852 mL |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.137 mL |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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Ostarine and Ligandrol Improve Muscle Tissue in an Ovariectomized Rat Model
Front Endocrinol (Lausanne) 2020 Sep 17;11:556581.PMID:33042018DOI:10.3389/fendo.2020.556581.
In postmenopausal women, hormonal decline changes muscle function and structure. The non-steroidal selective androgen receptor modulators (SARMs) Ostarine (OS) and Ligandrol (LG) have been shown to increase muscle mass and physical function while showing a relative low risk profile. Information about their effects on muscle structure and metabolism is lacking. To analyze this, two experiments were performed using ovariectomized rats as a standard model for postmenopausal conditions. In each experiment, 3-month old Sprague-Dawley rats were divided into five groups (n = 12 to 15). One group remained intact (Non-OVX), the other four groups were ovariectomized (OVX) and remained untreated for eight (OS Experiment) or nine (LG Experiment) weeks. Thereafter, rats of three of the four OVX groups were treated with OS or LG (with doses of 0.04, 0.4, or 4 mg/kg body weight/day) for 5 weeks. Then, uterus, gastrocnemius, and soleus muscles were weighed, fiber size, capillary density, and enzyme activity (lactate dehydrogenase [LDH], citrate synthase [CS], and complex I) were analyzed. In the LG experiment, intramuscular fat content was determined in the quadriceps femoris muscle. All OS treatments resulted in a higher capillary density in the gastrocnemius and longissimus muscles compared with the Non-OVX and the OVX rats, whereas all LG treatments showed a higher capillary density compared with the Non-OVX group. Muscle fiber size and distribution patterns were not changed under either SARM. The CS activity was higher in the longissimus muscle under OS treatment. LG resulted in a higher activity of CS in the gastrocnemius and of LDH in the longissimus muscle. Both SARMs showed an uterotrophic effect, OS at 4 and 0,4 mg dosages, LG at 4 mg dosage. In sum, beneficial effect on muscle vascularization was observed for both SARMs with a stronger impact for OS. LG showed more effect on muscle metabolism. However, a higher muscle weight and intramuscular fat content observed after LG treatment (4 mg) as well as an uterotrophic effect of both SARMs at higher dosages could be considered as an unfavorable side effects and might be a limitation for their application at these dosages.
Effect of Ostarine (enobosarm/GTX024), a selective androgen receptor modulator, on adipocyte metabolism in Wistar rats
J Physiol Pharmacol 2019 Aug;70(4).PMID:31642815DOI:10.26402/jpp.2019.4.04.
Synthetic ligands of androgen receptor (AR) are a standard in the treatment of androgen deficiency. One of the effects of androgen deficiency is the disturbance in the homeostasis of lipid metabolism. Till date, there are no effective compounds developed to treat androgen deficiency without having any side effects. Nonsteroidal selective androgen receptor modulators (SARMs) are a promising solution for various clinical indications. In this study, we investigated the effect of Ostarine (enobosarm), a nonsteroidal SARM, on the rat adipocyte metabolism using in vitro techniques. Isolated rat adipocytes were incubated in the presence of different concentrations of Ostarine. Control incubation with testosterone as the natural ligand for AR was performed. AR inhibitors were used to investigate the genomic activity of Ostarine. Changes in the intensity of lipolysis, lipogenesis, and the secretion of leptin and adiponectin were measured. Moreover, the gene expression of leptin and adiponectin was assessed. For the first time, we have shown that Ostarine has a significant effect on the intensity of lipid metabolism. Ostarine downregulates the expression of leptin and adiponectin mRNAs, as well as decreases their release from rat adipocytes. According to our results, Ostarine acts via AR with a similar effect as testosterone in the regulation of lipid metabolism and endocrine function of mature rat adipocytes in vitro. Our results indicate the need for further studies on the effects of SARM on the whole organism.
Ostarine-Induced Myogenic Differentiation in C2C12, L6, and Rat Muscles
Int J Mol Sci 2022 Apr 15;23(8):4404.PMID:35457222DOI:10.3390/ijms23084404.
Ostarine (also known as enobosarm or Gtx-024) belongs to the selective androgen receptor modulators (SARMs). It is a substance with an aryl-propionamide structure, classified as a non-steroidal compound that is not subjected to the typical steroid transformations of aromatization and reduction by α5 reductase. Despite ongoing research on Ostarine, knowledge about it is still limited. Earlier studies indicated that Ostarine may affect the metabolism of muscle tissue, but this mechanism has not been yet described. We aimed to investigate the effect of Ostarine on the differentiation and metabolism of muscle. Using C2C12 and L6 cells, as well as muscles obtained from rats administered Ostarine, we showed that Ostarine stimulates C2C12 and L6 proliferation and cell viability and that this effect is mediated by androgen receptor (AR) and ERK1/2 kinase activation (p < 0.01). We also found that Ostarine stimulates muscle cell differentiation by increasing myogenin, MyoD, and MyH expression in both types of cells (p < 0.01). Moreover, pharmacological blocking of AR inhibits the stimulatory effect of Ostarine. We further demonstrated that 30 days of Ostarine administration increases myogenin, MyoD, and MyH expression, as well as muscle mass, in rats (p < 0.01). Based on our research, we conclude that Ostarine stimulates muscle tissue proliferation and differentiation via the androgen receptor.
Drug-Induced Liver Injury From Enobosarm (Ostarine), a Selective Androgen Receptor Modulator
ACG Case Rep J 2021 Jan 7;8(1):e00518.PMID:34368386DOI:10.14309/crj.0000000000000518.
Anabolic steroids are well-known to cause liver injury, which may manifest with jaundice and elevated liver enzymes. Selective androgen receptor modulators (SARMs) have been developed to enhance muscle bulk without the side effects associated with exogenous androgen steroids. We report a case of significant cholestatic liver injury associated with a SARM, Ostarine (enobosarm), similar to that associated with anabolic steroids. Liver injury from SARMs has not been reported frequently, and we speculate that this may be seen more often as the consumption of SARMs increases in the athletic market.
Ostarine attenuates pyocyanin in Pseudomonas aeruginosa by interfering with quorum sensing systems
J Antibiot (Tokyo) 2021 Dec;74(12):863-873.PMID:34480092DOI:10.1038/s41429-021-00469-4.
Antimicrobial resistance has been an increasingly serious threat to global public health. Anti-virulence strategies are being developed to manage antibiotic resistance because they apply a lower selective pressure for antimicrobial-resistant pathogens than that created using traditional bactericides. We aimed to discover novel small molecules that can reduce the production of virulence factors in Pseudomonas aeruginosa and determine the mechanism of action underlying these effects. A clinical compound library was screened, and Ostarine was identified as a potential anti-virulence agent. The effects of Ostarine were studied via antimicrobial susceptibility testing, bacterial growth assays, pyocyanin quantitation assays, transcriptomic analysis, quorum sensing signal molecule quantification, and real-time PCR assays. Ostarine treatment significantly decreased the synthesis of pyocyanin without any bactericidal action. Besides, Ostarine treatment did not affect the relative growth rate and cell morphology of bacteria. Treatment with Ostarine interfered with quorum sensing by decreasing the transcription of genes associated with quorum sensing systems and the production of signalling molecules. The inhibition of Ostarine on pyocyanin production and gene expression can be alleviated when signalling molecules were supplemented externally. Overall, Ostarine may act as a novel anti-virulence agent that can attenuate P. aeruginosa pyocyanin by interfering with quorum sensing systems.