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CGP-53153 Sale

目录号 : GC32422

CGP-53153是甾体类的5alphareductase抑制剂,在大鼠和人前列腺组织中的IC50值分别为36nM。

CGP-53153 Chemical Structure

Cas No.:149281-19-6

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1mg
¥1,785.00
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5mg
¥3,570.00
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10mg
¥6,069.00
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20mg
¥10,710.00
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Sample solution is provided at 25 µL, 10mM.

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.

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

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].

[1]. H?usler A, et al. CGP-53153: a new potent inhibitor of 5alpha-reductase. J Steroid Biochem Mol Biol. 1996 Feb;57(3-4):187-95.

实验参考方法

Animal experiment:

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:

[1]. H usler A, et al. CGP-53153: a new potent inhibitor of 5alpha-reductase. J Steroid Biochem Mol Biol. 1996 Feb;57(3-4):187-95.

化学性质

Cas No. 149281-19-6 SDF
Canonical SMILES C[C@@]1([C@H]2C(NC(C)(C)C#N)=O)[C@](CC2)([H])[C@@](CC[C@](N3)([H])[C@@]4(C=CC3=O)C)([H])[C@]4([H])CC1
分子式 C23H33N3O2 分子量 383.53
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6074 mL 13.0368 mL 26.0736 mL
5 mM 0.5215 mL 2.6074 mL 5.2147 mL
10 mM 0.2607 mL 1.3037 mL 2.6074 mL
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