| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: =99.94%
| Targets |
GSK-2881078 targets the androgen receptor (AR), a nuclear receptor that regulates gene expression in response to androgens. As a SARM, it selectively activates AR in muscle and bone with tissue-specific effects, promoting anabolic effects while minimizing androgenic effects in prostate and other tissues.
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| ln Vitro |
GSK-2881078 activates AR signaling with EC50 values characterized in cell-based assays (EC50 = 4.44 nM in certain systems). It promotes muscle mass and bone density in preclinical models. The compound has potential applications in treating muscle weakness and cachexia associated with chronic and acute illness.
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| ln Vivo |
In vivo, GSK-2881078 has been studied for its potential to treat muscle wasting and cachexia. As a SARM, it promotes anabolic effects in muscle and bone while minimizing prostate-related side effects. The compound has been evaluated in preclinical models of muscle weakness and cachexia.
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| Enzyme Assay |
Cell-free AR binding assays for GSK-2881078 utilize purified recombinant androgen receptor ligand-binding domain. Binding affinity is measured using radiolabeled [3H]-DHT competition binding or fluorescence polarization. The compound's selectivity for AR over other nuclear receptors is assessed. Transactivation assays use AR-responsive reporter gene constructs in cell-free systems.
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| Cell Assay |
Cells expressing AR (e.g., C2C12 myoblasts, LNCaP prostate cancer cells) are treated with GSK-2881078 at various concentrations. AR target gene expression (e.g., myostatin, IGF-1, PSA) is assessed by qRT-PCR. Muscle cell differentiation and fusion are evaluated by microscopy and myosin heavy chain expression. Androgenic effects in prostate cells are assessed as a measure of selectivity.
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| Animal Protocol |
In vivo animal studies for GSK-2881078 are conducted in rodent models of muscle wasting and cachexia. The compound is administered orally. Muscle mass (gastrocnemius, tibialis anterior), grip strength, and bone density are measured. Androgenic effects in prostate and other tissues are assessed. Pharmacodynamic markers (AR target gene expression) are measured in muscle and other tissues.
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| ADME/Pharmacokinetics |
GSK-2881078 is orally bioavailable. As a small molecule (MW 330.33, formula C14H13F3N2O2S), it has favorable drug-like properties for oral administration. The compound is soluble in DMSO (33 mg/mL). PK parameters including Tmax, half-life, clearance, and bioavailability have been characterized in preclinical species.
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| Toxicity/Toxicokinetics |
Toxicity data for GSK-2881078 are limited. As a SARM, the compound is designed to have a favorable safety profile compared to traditional androgens, with reduced prostate-related side effects. Standard toxicological assessments including genotoxicity, reproductive toxicity, and chronic toxicity studies would be required for development. Hepatic effects are a potential concern with SARMs.
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| References |
https://newdrugapprovals.org/2016/06/14/gsk-2881078/
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| Additional Infomation |
GSK-2881078 (molecular formula C14H13F3N2O2S, MW 330.33) is a nonsteroidal selective androgen receptor modulator (SARM) developed by GlaxoSmithKline. It activates AR signaling in muscle and bone to promote anabolic effects while minimizing prostate-related side effects. The compound has potential applications in treating muscle weakness and cachexia.
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| Molecular Formula |
C14H13F3N2O2S
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|---|---|
| Molecular Weight |
330.3254
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| Exact Mass |
330.064
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| CAS # |
1539314-06-1
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| PubChem CID |
86709174
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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 |
521.6±50.0 °C at 760 mmHg
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| Flash Point |
269.3±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.555
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| LogP |
2.23
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
561
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](CS(=O)(=O)C)N1C=CC2=C1C=CC(=C2C(F)(F)F)C#N
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| InChi Key |
PUZZHQYLIBUVEY-SECBINFHSA-N
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| InChi Code |
InChI=1S/C14H15F3N2O2S/c1-9(8-22(2,20)21)19-6-5-11-12(19)4-3-10(7-18)13(11)14(15,16)17/h3-4,9H,5-6,8H2,1-2H3/t9-/m1/s1
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| Chemical Name |
(R)-1 -(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile
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| Synonyms |
GSK2881078; GSK 2881078; GSK-2881078.
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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 |
| 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) |
DMSO : ≥ 33 mg/mL (~99.90 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0273 mL | 15.1364 mL | 30.2728 mL | |
| 5 mM | 0.6055 mL | 3.0273 mL | 6.0546 mL | |
| 10 mM | 0.3027 mL | 1.5136 mL | 3.0273 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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