LGD-3303
Based on 4 publication(s) in Google Scholar
LGD-3303 is a selective androgen receptor modulator (SARM).
For research use only. We do not sell to patients.
- Purity : 99.57%
- CAS No.: 917891-35-1
- Formula: C16H14ClF3N2O
- Molecular Weight:342.74
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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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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LGD-3303 (Standard)Reference Standard
Publications Citing Use of MedChemExpress (MCE) LGD-3303
More
Biological Activity
Description
IC50 & Target
SARM[1]
In Vitro
LGD-3303 is a nonsteroidal, nonaromatizable androgen receptor ligand that binds to the androgen receptor with high affinity in a radiolabeled to competitive binding assay (Ki=0.9 nM). LGD-3303 binds to the mineralocorticoid, glucocorticoid, and progesterone receptors with greatly reduces affinity in comparison with the androgen receptor (Ki=1261, 581, and 136 nM, respectively). LGD-3303 potently activates transcription through the androgen receptor (EC50=3.6 nM) and has 134% efficacy relative to the steroidal androgen Dihydrotestosterone (DHT)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 917891-35-1
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Appearance Solid
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Molecular Weight 342.74
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Formula C16H14ClF3N2O
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Color White to yellow
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SMILES
O=C1NC2=C(C3=C(N(CC(F)(F)F)C(CC)=C3C)C=C2)C(Cl)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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J Pharm Biomed Anal
Equine in vivo metabolite profiling of the selective androgen receptor modulator LGD-3303 for doping control. [Abstract]2023 Sep 5:233:115468. PMID: 37224728 -
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 -
Drug Test Anal
Analysis of supplements available to UK consumers purporting to contain selective androgen receptor modulators. [Abstract]2021 Jan;13(1):122-127. PMID: 32748554
Solvent & Solubility
In Vitro:
DMSO : 10.42 mg/mL (30.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: 1.04 mg/mL (3.03 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.04 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 (10.4 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.
In Vivo Dissolution Calculator
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.
Protocols
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
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Data Sheet (283 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]. Vajda EG, et al. Combination treatment with a selective androgen receptor modulator q(SARM) and a bisphosphonate has additive effects in osteopenic female rats. J Bone Miner Res. 2009 Feb;24(2):231-40. [Content Brief]
[2]. Vajda EG, et al. Pharmacokinetics and pharmacodynamics of LGD-3303 [9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an orally available nonsteroidal-selective androgen receptor modulator. J Pharmacol Exp Ther. 2009 Feb;328(2):663-70. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9177 mL | 14.5883 mL | 29.1766 mL | 72.9416 mL |
| 5 mM | 0.5835 mL | 2.9177 mL | 5.8353 mL | 14.5883 mL | |
| 10 mM | 0.2918 mL | 1.4588 mL | 2.9177 mL | 7.2942 mL | |
| 15 mM | 0.1945 mL | 0.9726 mL | 1.9451 mL | 4.8628 mL | |
| 20 mM | 0.1459 mL | 0.7294 mL | 1.4588 mL | 3.6471 mL | |
| 25 mM | 0.1167 mL | 0.5835 mL | 1.1671 mL | 2.9177 mL | |
| 30 mM | 0.0973 mL | 0.4863 mL | 0.9726 mL | 2.4314 mL |
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