CGP-53153
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。
Cas No.:149281-19-6
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet