[CAS NO. 627530-84-1] BMS-564929
PRODUCTS SPECIFICATIONS [627530-84-1]
DESCRIPTION [627530-84-1]
Overview
| MDL | MFCD15146692 |
|---|---|
| Molecular Weight | 305.72 |
| Molecular Formula | C14H12ClN3O3 |
| SMILES | N#CC1=CC=C(N(C(N2[C@@]3([H])[C@H](O)CC2)=O)C3=O)C(C)=C1Cl |
4 Publications Citing Use of MCE
Summary
BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a K i of 2.11±0.16 nM.
IC50 & Target
Ki: 2.11±0.16 nM (Androgen receptor) [1]
In Vitro
BMS-564929 exhibits a potency (EC 50 , calculated as the concentration at which 50% of the maximum stimulatory effect of DHT is achieved) of 0.44±0.03 nM in the C2C12 myoblast cell line. In the PEC cell line, the EC 50 for BMS-564929 is 8.66±0.22 nM. BMS-564929 is more than 1000-fold selective for AR vs. estrogen receptors (ER) α and β, glucocorticoid receptor (GR), and mineralocorticoid receptor (MR), and approximately 400-fold selective vs. progesterone receptor (PR). BMS-564929 shows no measurable activity in functional transactivation assays with ERα/β, GR, MR, or PR at concentrations up to 30 μM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In sexually mature, castrated male rats, a well-characterized animal model, BMS-564929 (p.o.) shows substantially more potent activity in the levator ani, exhibiting an ED 50 of 0.0009 mg/kg in the levator ani and an ED 50 of 0.14 mg/kg in the prostate; a net 160-fold selectivity for muscle vs. prostate. Approximately 100% muscle stimulation is achieved at 0.1 mg/kg, reaching greater than 125% stimulation at 0.3 and 1 mg/kg. Compared with T propionate (TP) in the same model, BMS-564929 is more than 200 times more potent in stimulation of muscle and 80 times more selective for muscle vs. prostate [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 163.55 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2710 mL | 16.3548 mL | 32.7097 mL |
| 5 mM | 0.6542 mL | 3.2710 mL | 6.5419 mL |
| 10 mM | 0.3271 mL | 1.6355 mL | 3.2710 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.18 mM); Clear solution
Synonyms
