| 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 |
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LY2452473 is a novel, potent, selective and orally bioavailable androgen receptor modulator (SARM) that is strong, selective, and orally bioavailable. It may also have tissue-specific androgenic/anti-androgenic effects. In certain tissues and organs, such as the penis, skeletal muscle, and bone, LY2452473 functions as an agonist by binding to and activating the androgen receptor (AR); in the prostate, on the other hand, it functions as an antagonist by preventing both AR activation and AR-mediated cellular proliferation. While not promoting prostate growth, this may help with erectile dysfunction, bone formation, and muscle mass and strength.
| Targets |
Androgen receptor
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|---|---|
| ln Vivo |
LY2452473 is a selective androgen receptor modulator under development to treat hypogonadism-related illnesses. LY2452473 is cleared slowly (plasma terminal t1/2 of 51 h for the total radioactivity and 27 h for LY2452473) and absorbed quickly (time to reach maximum plasma concentration for both LY2452473 and total radioactivity is 2-3 h)[1].
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| References |
| Molecular Formula |
C22H22N4O2
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|---|---|
| Molecular Weight |
374.435684680939
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| Exact Mass |
374.17
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| Elemental Analysis |
C, 70.57; H, 5.92; N, 14.96; O, 8.55
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| CAS # |
1029692-15-6
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| Related CAS # |
1029692-15-6
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| Appearance |
Solid powder
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| SMILES |
CC(C)OC(=O)N[C@H]1CC2=C(C1)N(C3=C2C=C(C=C3)C#N)CC4=CC=CC=N4
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| InChi Key |
IHIWYQYVBNODSV-KRWDZBQOSA-N
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| InChi Code |
InChI=1S/C22H22N4O2/c1-14(2)28-22(27)25-17-10-19-18-9-15(12-23)6-7-20(18)26(21(19)11-17)13-16-5-3-4-8-24-16/h3-9,14,17H,10-11,13H2,1-2H3,(H,25,27)/t17-/m0/s1
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| Chemical Name |
propan-2-yl N-[(2S)-7-cyano-4-(pyridin-2-ylmethyl)-2,3-dihydro-1H-cyclopenta[b]indol-2-yl]carbamate
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| Synonyms |
LY2452473; LY 2452473; LY-2452473
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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: ~62.5 mg/mL (~166.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6707 mL | 13.3533 mL | 26.7065 mL | |
| 5 mM | 0.5341 mL | 2.6707 mL | 5.3413 mL | |
| 10 mM | 0.2671 mL | 1.3353 mL | 2.6707 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01275157 | Completed | Drug: LY2452473 | Healthy Volunteers | Eli Lilly and Company | January 2011 | Phase 1 |
| NCT01401543 | Completed | Drug: LY2452473 Drug: Tadalafil |
Erectile Dysfunction | Eli Lilly and Company | July 2011 | Phase 1 |
| NCT02499497 | Completed | Drug: LY2452473 Drug: Placebo |
Prostate Cancer | Dana-Farber Cancer Institute | February 29, 2016 | Phase 2 |
| NCT01160289 | Completed | Drug: LY2452473 Drug: tadalafil |
Erectile Dysfunction | Eli Lilly and Company | October 2010 | Phase 2 |
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