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Purity: ≥98%
LGD-3303 is a potent, selective, orally bioavailable, and non-sterdoidal androgen receptor modulator (SARM) with anabolic effects on muscle and cortical bone not observed with bisphosphonates. It shows little or no cross-reactivity with related nuclear receptors. Upon oral administration of LGD-3303 for 14 days in orchidectomized male rats, the tissue selective activity of LGD-3303 was assessed, and LGD-3303 was found to increase the levator ani muscle weight above eugonadal levels but had greatly reduced activity on the prostate, never increasing the ventral prostate weight to >50% of eugonadal levels even at high doses.LGD-3303 increased muscle weight in females rats. In addition, LGD-3303 increased BMD and BMC at both cortical and cancellous bone sites. At cortical sites, the effects were caused in part by anabolic activity on the periosteal surface.
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| References |
J Bone Miner Res.2009 Feb;24(2):231-40.
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| Molecular Formula |
C16H14CLF3N2O
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| Molecular Weight |
342.75
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| CAS # |
917891-35-1
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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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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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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 | 2.9176 mL | 14.5879 mL | 29.1758 mL | |
| 5 mM | 0.5835 mL | 2.9176 mL | 5.8352 mL | |
| 10 mM | 0.2918 mL | 1.4588 mL | 2.9176 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.
In ORDX male rats, testosterone increased levator ani muscle (LA) weight at doses that have equivalent effects on ventral prostate (VP) weight, indicating a lack of tissue selectivity.J Bone Miner Res.2009 Feb;24(2):231-40. |
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LGD‐3303 increases body and gastrocnemius muscle weight in OVX female rats after 12 wk of treatment.J Bone Miner Res.2009 Feb;24(2):231-40. |
LGD‐3303 increases lumbar spine and femoral BMD and BMC in OVX female rats.J Bone Miner Res.2009 Feb;24(2):231-40. |
(A) Photomicrograph of the periosteal surface of the midfemoral diaphysis viewed under epifluorescent light. (B) LGD‐3303 increases periosteal bone formation at the midfemoral diaphysis in OVX female rats. Alendronate has no activity at this site.J Bone Miner Res.2009 Feb;24(2):231-40. |
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Estrogen deficiency in female rats increases lumbar spine cancellous bone formation rate.J Bone Miner Res.2009 Feb;24(2):231-40. |
Three‐point bending test of the femur and compression test of the lumbar vertebral body.J Bone Miner Res.2009 Feb;24(2):231-40. |
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