Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H22N4O2 |
Molecular Weight | 374.4357 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)OC(=O)N[C@@H]1CC2=C(C1)C3=C(C=CC(=C3)C#N)N2CC4=CC=CC=N4
InChI
InChIKey=IHIWYQYVBNODSV-KRWDZBQOSA-N
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
Molecular Formula | C22H22N4O2 |
Molecular Weight | 374.4357 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
LY2452473 is a selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity. Upon oral administration, LY2452473 acts as an agonist in select tissues and organs, including skeletal muscle, bone and the penis, thereby binding to and activating androgen receptor (AR) while acting as an antagonist in the prostate, thereby blocking AR activation and AR-mediated cellular proliferation. This may improve muscle mass and strength, bone formation, and erectile dysfunction while not stimulating growth of the prostate. Eli Lilly was developing LY 2452473/tadalafil combination for the treatment of erectile dysfunction. In addition, Eli Lilly is studying the use of a targeted LY 2452473 therapy, as a possible improvement in quality of life for prostate cancer patients who have undergone radical prostatectomy.
Originator
Approval Year
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 03:21:10 GMT 2023
by
admin
on
Sat Dec 16 03:21:10 GMT 2023
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Record UNII |
XKW9MYF94Y
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Record Status |
Validated (UNII)
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Record Version |
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C123792
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100000175545
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24963749
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1029692-15-6
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CHEMBL3542265
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XKW9MYF94Y
Created by
admin on Sat Dec 16 03:21:10 GMT 2023 , Edited by admin on Sat Dec 16 03:21:10 GMT 2023
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DTXSID50145591
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DB12573
Created by
admin on Sat Dec 16 03:21:10 GMT 2023 , Edited by admin on Sat Dec 16 03:21:10 GMT 2023
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LY-2452473
Created by
admin on Sat Dec 16 03:21:10 GMT 2023 , Edited by admin on Sat Dec 16 03:21:10 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE |
After normalization for hepatic content of the contributing P450s, CYP3A4 was the largest contributor (68%) to substrate depletion, suggesting a major role of CYP3A4 in the hepatic clearance of LY2452473.
MAJOR
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TARGET -> AGONIST |
SARM
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METABOLIC ENZYME -> SUBSTRATE |
. CYP2J2 showed the second largest contribution to substrate depletion (15%) after normalization for hepatic content
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE -> PARENT |
MAJOR
PLASMA
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METABOLITE -> PARENT |
FECAL; PLASMA; URINE
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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