CGP-53153
Names
Biological Activity
[Description]:
CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.
[Related Catalog]:
[Target]
IC50: 36 nM (rat 5 alpha reductase), 262 nM (human 5 alpha reductase)[1]
[In Vitro]
CGP-53153 competitively inhibits rat microsomal 5 alpha reductase from prostate with an IC50 of 36 nM compared to the reference compound finasteride (IC50=11 nM). CGP 53153 is approximately one order of magnitude more potent in inhibiting rat compared to human 5 alpha reductase, with IC50 values of 36 and 262 nM, respectively
[In Vivo]
CGP-53153 can significantly reduce T-propionate-mediated prostate growth at oral doses of 0.01 mg/kg. CGP-53153 significantly reduces prostate weight at 3 and 10 mg/kg by 31% and 37%, respectively. Treatment for 12 weeks with both CGP-53153 reduces prostate volume by more than 70% in individual dogs. Neither body weight nor the weight of any organ tested is affected by CGP-53153[1].
[Animal admin]
Rats: Adult male rats weighing 160-180 g at the start of the study are treated orally once daily for 14 consecutive days either with increasing doses of CGP-53153 (1, 3 and 10 mg/kg) or with 10 mg/kg finasteride in 20% HCD. Control rats are given 20% HCD. On the 14th treatment day, 4 h after the last application, the animals are randomized and rapidly killed. Trunk blood is collected in polystyrene tubes and serum obtained by centrifugation is stored at -20°C for hormone (T, DHT and rat-LH) determination at a later date. After decapitation, the following organs are excised and weighed after removal of adhering fat and connective tissue: ventral prostate, seminal vesicles, levator ani and bulbocavernosus muscle, testes, pituitary, adrenals, thyroid, thymus and liver[1].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C23H33N3O2
[ Molecular Weight ]:
383.52700
[ Exact Mass ]:
383.25700
[ PSA ]:
81.99000
[ LogP ]:
4.03788
[ Storage condition ]:
2-8℃