| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
LGD-2226 selectively targets the human androgen receptor (AR). It binds to the AR with high affinity, exhibiting a Ki of 1 nM and an EC50 of 0.2 nM. As a SARM, it acts as a tissue-selective agonist, promoting anabolic effects in muscle and bone while having reduced effects on the prostate compared to traditional androgens. Its mechanism of action involves modulating the transcription of androgen-responsive genes in a tissue-specific manner, mediated by its interaction with the AR.
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| ln Vitro |
In vitro, LGD-2226 binds to the human androgen receptor with high potency, showing a Ki of 1 nM and an EC50 of 0.2 nM. This indicates that it is a full agonist at the AR in cell-based reporter assays. Its selectivity is demonstrated by its lack of significant activity at other steroid hormone receptors, including the glucocorticoid, progesterone, mineralocorticoid, and estrogen receptors. These in vitro activities confirm its profile as a potent and selective SARM.
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| ln Vivo |
In vivo, LGD-2226 has demonstrated tissue selectivity in animal models. It shows anabolic effects on muscle, promoting muscle growth, while having reduced effects on the prostate compared to testosterone. This tissue-selective profile is the hallmark of a SARM and is the basis for its potential therapeutic use in conditions like muscle wasting and osteoporosis, where anabolic effects are desired without the unwanted androgenic side effects on the prostate.
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| Enzyme Assay |
Non-cell-based assays for LGD-2226 typically involve radioligand binding assays using the human androgen receptor. The receptor is incubated with a radiolabeled androgen (e.g., [3H]-DHT) and varying concentrations of LGD-2226. The compound's ability to displace the radiolabeled ligand is measured, and its binding affinity (Ki) is determined. Selectivity is determined by performing similar binding assays against other steroid receptors.
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| Cell Assay |
Cellular assays for LGD-2226 are performed using cells that express the human androgen receptor, such as the HEK293 or CV-1 cell line, transfected with an androgen-responsive reporter gene. The cells are treated with LGD-2226 at various concentrations, and the reporter gene activity (e.g., luciferase) is measured. The EC50, the concentration required to achieve 50% of the maximum activation, is determined. These functional assays confirm that LGD-2226 acts as an agonist at the AR.
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| Animal Protocol |
In vivo animal models for LGD-2226 typically involve the use of orchidectomized (castrated) rats, which have low endogenous androgen levels. The animals are administered LGD-2226 orally at various doses. The compound's effect on muscle mass (e.g., levator ani muscle weight) and prostate weight is measured. The ratio of muscle to prostate weight is used as an indicator of tissue selectivity.
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| ADME/Pharmacokinetics |
LGD-2226 has a molecular weight of 413.28 g/mol and a molecular formula of C21H17F6N3O. It is orally active, indicating good bioavailability. The compound is soluble in DMSO. Detailed PK parameters such as half-life and volume of distribution are not extensively detailed in the provided search results. It is typically stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for LGD-2226 are not provided in the search results. As a SARM, its safety profile would be a key consideration for therapeutic development. Potential side effects could include effects on lipid profiles, liver function, and, depending on its selectivity, androgenic side effects. The compound is intended for research use only and is not for human consumption.
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| Additional Infomation |
androgen receptor modulators.
LGD-2226 is a selective and orally active androgen receptor modulator. It exhibits a Ki of 1 nM and an EC50 of 0.2 nM for the human androgen receptor, with >1000-fold selectivity over other steroid receptors. It shows tissue selectivity in animal models and is being studied for muscle wasting, osteoporosis, and sexual dysfunction. It has the CAS number 328947-93-9 and is supplied for research purposes. |
| Molecular Formula |
C14H9F9N2O
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|---|---|
| Molecular Weight |
392.2246
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| Exact Mass |
392.057
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| CAS # |
328947-93-9
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| PubChem CID |
11560224
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| Appearance |
Light yellow to green yellow solid powder
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| LogP |
4.89
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
548
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(CN(C1C=CC2=C(C(C(F)(F)F)=CC(N2)=O)C=1)CC(F)(F)F)(F)F
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| InChi Key |
ULBPQWIGZUGPHU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H9F9N2O/c15-12(16,17)5-25(6-13(18,19)20)7-1-2-10-8(3-7)9(14(21,22)23)4-11(26)24-10/h1-4H,5-6H2,(H,24,26)
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| Chemical Name |
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1H-quinolin-2-one
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| Synonyms |
LGD 2226 LGD2226 LGD-2226
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5496 mL | 12.7479 mL | 25.4959 mL | |
| 5 mM | 0.5099 mL | 2.5496 mL | 5.0992 mL | |
| 10 mM | 0.2550 mL | 1.2748 mL | 2.5496 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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