L-AP4
(Synonyms: L(+)-2-氨基-4-膦酰基丁酸,L-APB) 目录号 : GC17932A selective Group III metabotropic glutamate receptor agonist
Cas No.:23052-81-5
Sample solution is provided at 25 µL, 10mM.
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L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
Paw withdrawal threshold in response to application of von Frey filaments before spinal nerve ligation is 22.6±2.4 g. The mechanical threshold decreases significantly (2.3±0.5 g, P<0.05) within 10 days after nerve ligation and remains stable for at least 8 weeks. Intrathecal injection of 5 to 30 μg of L-APB significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. The maximal effect of L-APB appears within 45 min and gradually subsided in 120 min following intrathecal administration[2].
References:
[1]. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989.
[2]. Chen SR, et al. Distinct roles of group III metabotropic glutamate receptors in control of nociception and dorsal horn neurons in normal and nerve-injured Rats. J Pharmacol Exp Ther. 2005 Jan;312(1):120-6.
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Animal experiment: |
Rats[2]The effect of L-APB (L-AP4: 5, 10, and 50 μM) on identified ascending dorsal horn neurons is studied in 20 L5 and L6 spinal nerve ligated rats. L-APB, starting with the lowest concentration, is applied topically onto the exposed spinal cord. Five to 10 min following L-APB application, the response of neurons to graded mechanical stimuli is re-examined. To ensure that the effect of L-APB on dorsal horn neurons is through group III mGluRs, the inhibitory effect of 50 μM L-APB is tested before and after topical application of 100 μM MAP4, a specific antagonist for group III mGluRs, in another 12 dorsal horn neurons. MAP4 is applied to the recording site 10 min before application of 50 μM L-APB. In addition, to determine whether topical application of L-APB affects ascending dorsal horn neurons in normal rats, the effect of 50 μM L-APB on spontaneous and evoked responses to graded mechanical stimuli is examined in 11 dorsal horn neurons from eight normal rats. Also, the effect of topical spinal application of 100 μM MAP4 alone on these cells is tested 15 to 20 min after washout of L-APB solution from the recording site[2]. |
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References: [1]. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989. |
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| Cas No. | 23052-81-5 | SDF | |
| 别名 | L(+)-2-氨基-4-膦酰基丁酸,L-APB | ||
| 化学名 | (S)-2-amino-4-phosphonobutanoic acid | ||
| Canonical SMILES | OP(O)(CC[C@@H](C(O)=O)N)=O | ||
| 分子式 | C4H10NO5P | 分子量 | 183.1 |
| 溶解度 | PBS (pH 7.2): 2 mg/ml | 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 | 5.4615 mL | 27.3075 mL | 54.615 mL |
| 5 mM | 1.0923 mL | 5.4615 mL | 10.923 mL |
| 10 mM | 0.5461 mL | 2.7307 mL | 5.4615 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