CGP 52432
(Synonyms: 4-苄氧基苯基异硫氰酸酯) 目录号 : GC16947
A GABAB receptor antagonist
Cas No.:139667-74-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice[2]Two separate cohorts of male pups are used for the study. One cohort is treated with either R(+)baclofen HCl (2 mg/kg) or with vehicle (PBS). The second cohort is treated with the GABAB receptor antagonist CGP52342 (10, 30 mg/kg) or vehicle (PBS). Drugs are freshly prepared for injection each day, by dissolution in PBS with vortexing and brief sonication. Doses of R(+)baclofen and CGP52432 are chosen to be well tolerated in adult mice. All drug treatments are given via subcutaneous injection, once daily from P14-28 in a volume of 0.05 mL[2]. |
References: [1]. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5. | |
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM, 35- and 100-fold lower than at the receptors regulating somatostatin and glutamate overflow, respectively[1].
CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze[2]. CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolishes the suppressive effects of GABA ( 50 μmol/kg, i.v.) on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, causeing elimination of the renoprotective effects of GABA in rats[3].
References:
[1]. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5.
[2]. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10.
[3]. Kobuchi S, et al. Mechanisms underlying the renoprotective effect of GABA against ischaemia/reperfusion-induced renal injury in rats. Clin Exp Pharmacol Physiol. 2015 Mar;42(3):278-86.
| Cas No. | 139667-74-6 | SDF | |
| 别名 | 4-苄氧基苯基异硫氰酸酯 | ||
| 化学名 | (S)-(3-((3,4-dichlorobenzyl)amino)propyl)(diethoxymethyl)phosphinic acid | ||
| Canonical SMILES | ClC1=CC(CNCCC[P@](O)(C(OCC)OCC)=O)=CC=C1Cl | ||
| 分子式 | C15H24Cl2NO4P | 分子量 | 384.24 |
| 溶解度 | <3.84mg/ml in Water | 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 | 2.6025 mL | 13.0127 mL | 26.0254 mL |
| 5 mM | 0.5205 mL | 2.6025 mL | 5.2051 mL |
| 10 mM | 0.2603 mL | 1.3013 mL | 2.6025 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。
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