1. Metabolic Enzyme/Protease
  2. 5 alpha Reductase
  3. CGP-53153

CGP-53153 

Cat. No.: HY-U00125
Handling Instructions

CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.

For research use only. We do not sell to patients.

CGP-53153 Chemical Structure

CGP-53153 Chemical Structure

CAS No. : 149281-19-6

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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.

IC50 & 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].

Molecular Weight

383.53

Formula

C₂₃H₃₃N₃O₂

CAS No.

149281-19-6

SMILES

C[[email protected]@]1([[email protected]]2C(NC(C)(C)C#N)=O)[[email protected]](CC2)([H])[[email protected]@](CC[[email protected]](N3)([H])[[email protected]@]4(C=CC3=O)C)([H])[[email protected]]4([H])CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

CGP-53153CGP53153CGP 531535 alpha Reductase5α-reductaseInhibitorinhibitorinhibit

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