CGP 71683 hydrochloride
(Synonyms: CGP71683A) 目录号 : GC10167
An antagonist of NPY receptor Y5
Cas No.:192322-50-2
Sample solution is provided at 25 µL, 10mM.
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CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes[1].
CGP71683 (15 nmol/rat, icv, twice daily) shows anorexigenic effect, reducing food intake and bady weight of fed rats. CGP71683 causes 3-times higher serum total T4 and 37% increase in free T4 in the fasted rats than in the fasted controls rats[2].
Reference：
[1]. Lecklin A, et al. Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br J Pharmacol. 2002 Apr;135(8):2029-37.
[2]. Costa-e-Sousa RH, et al. Central NPY-Y5 receptors activation plays a major role in fasting-induced pituitary-thyroid axis suppression in adult rat. Regul Pept. 2011 Nov 10;171(1-3):43-7.
Animal experiment: | Rats[2]CGP71683 is dissolved in 30% DMSO and kept frozen at -20°C until the experiment. Each microinjection consists of 2 μL of either vehicle (30% DMSO) or CGP71683 (7.5 nmol/μL; 15 nmol/rat) injected during 30-60 s through the guide cannula, as the following protocols: I - rats with free access to chow receive 6 microinjections (15 nmol/rat, 10-14 h interval between each one) and are killed 1 h after the last injection, between 9 and 10 a.m. Food intake is estimated by the reduction in chow mass (g), evaluated daily, immediately before each icv injection. II - 72 h-fasted rats receive a single microinjection of vehicle or CGP71683 (15 nmol/rat) and sacrificed 1 h latter. III - during a period of 72 h of fasting, rats are treated with multiple injections of vehicle or CGP71683 with the same protocol used for fed animals, and the fasting period started 10 h before the first microinjection. At the end of experimental protocols, rats are decapitated and serum is obtained from trunk blood for the measurement of the concentrations of hormones[2]. |
References: [1]. Lecklin A, et al. Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br J Pharmacol. 2002 Apr;135(8):2029-37. | |
| Cas No. | 192322-50-2 | SDF | |
| 别名 | CGP71683A | ||
| 化学名 | N-(((1r,4r)-4-(((4-aminoquinazolin-2-yl)amino)methyl)cyclohexyl)methyl)naphthalene-1-sulfonamide hydrochloride | ||
| Canonical SMILES | O=S(NC[C@@H]1CC[C@@H](CNC2=NC(N)=C3C(C=CC=C3)=N2)CC1)(C4=CC=CC5=CC=CC=C45)=O.Cl | ||
| 分子式 | C26H29N5O2S.HCl | 分子量 | 512.07 |
| 溶解度 | <51.21mg/ml 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 | 1.9529 mL | 9.7643 mL | 19.5286 mL |
| 5 mM | 0.3906 mL | 1.9529 mL | 3.9057 mL |
| 10 mM | 0.1953 mL | 0.9764 mL | 1.9529 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet