Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C14H12ClN3O3 |
| Molecular Weight | 305.716 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C=CC(C#N)=C1Cl)N2C(=O)[C@@H]3[C@H](O)CCN3C2=O
InChI
InChIKey=KEJORAMIZFOODM-PWSUYJOCSA-N
InChI=1S/C14H12ClN3O3/c1-7-9(3-2-8(6-16)11(7)15)18-13(20)12-10(19)4-5-17(12)14(18)21/h2-3,10,12,19H,4-5H2,1H3/t10-,12+/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/17008401Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/18270691 |
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17008401
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/18270691 |
BMS-564929 is an investigational selective androgen receptor modulator, which is being developed by Bristol-Myers Squibb for treatment of the symptoms of age-related decline in androgen levels in men ("andropause"). Bristol-Myers Squibb presented data for BMS 564929 that showed favorable pharmacokinetics and the potential for use at a very low dose (0.03mg).
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17008401 |
2.11 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Determination of benzimidazole- and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS. | 2008-05 |
|
| Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats. | 2007-01 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17008401
Sprague Dawley rats (42–56 d old, 200–250 g) were dosed once daily by oral gavage with BMS-564929 (0.00001–10 mg/kg) in solution/suspension of 80% PEG 400 and 20% Tween 20 for 14 d.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17008401
The human cancer epithelial breast cell lines MDA MB-453 and T47D, were used for radioligand competition binding assays. Binding assays were conducted by incubating BMS-564929 at various concentrations with either [3H]DHT or [3H]progesterone with the cells for 2 h at room temperature. BMS-564929 is a high affinity ligand for AR with a Ki of 2.11 ± 0.16 nm
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WIKIPEDIA |
Designer-drugs-BMS-564929
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ACTIVE MOIETY