Lu AF21934
目录号 : GC15992
A positive allosteric modulator of mGluR4
Cas No.:1445605-23-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: Lu AF21934 is dispersed in 20% (2-hydropropyl)-b-cyclodextrin and are administered subcutaneously (s.c.) 60 min before the test. Lu AF21934 (2, 5, 10 and 15 mg/kg, s.c.) and diazepam (5 mg/kg, i.p.) are administered acutely 1 h before the Vogel’s conflict test. The effects of each drug in all experiments are measured in groups of 8-10 animals[1]. Mice: Lu AF21934 is dispersed in 20% (2-hydropropyl)-b-cyclodextrin and are administered subcutaneously (s.c.) 60 min before the test. Mice are gently placed into the box and allowed to explore for 15 s. Then, each time a mouse passed from one plate to another, the experimenter electrifies the whole floor thus evoking a visible flight reaction of the animal. If the animal continues running, no new shock is delivered for the following 3 s[1]. |
References: [1]. Sławińska A, et al. Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu₄ receptor. Neuropharmacology. 2013 Mar;66:225-35. | |
EC50: 500 nM
Lu AF21934 is a positive allosteric modulator of mGlu4 receptors.
The mGlu4 receptor subtype of the group III mGlu is mainly a presynaptic auto- or hetero-receptor. Its stimulation results in an inhibition of glutamatergic or GABAergic transmission and release
In vitro: Lu AF21934 has been identified as a brain-penetrating positive allosteric modulator of mGlu4 receptors. In broad in-vitro screens, Lu AF21934 could potentiate the glutamate response at the mGlu4 receptor with an Emax=120% and a glutamate fold-shift FS=5. Lu AF21934 did not showed any significant affinity for 70 GPCRs at 10 μM, but acted as a weak positive allosteric modulator of mGlu6 receptor, as well as an antagonist of adenosine A2A and 5-HT2B receptors [1].
In vivo: In rats, harmaline triggered tremor as manifested by an increase in the power within 9-15Hz band and in the tremor index. Harmaline also induced a biphasic effect on mobility, initially inhibiting the exploratory locomotor activity of rats, followed by an increase in their basic activity. Lu AF21934 at 0.5-5 mg/kg sc did not influence tremor but at doses of 0.5 and 2.5 mg/kg reversed harmaline-induced hyperactivity. MGlu4 mRNA expression was found to be high in the cerebellar cortex and low in the inferior olive [1].
Clinical trial: Up to now, Lu AF21934 is still in the preclinical development stage.
Reference:
[1] Ossowska K,Wardas J,Berghauzen-Maciejewska K,et al. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology.2014 Aug;83:28-35.
| Cas No. | 1445605-23-1 | SDF | |
| 化学名 | (1R,2S)-2-((3,4-dichlorophenyl)carbamoyl)cyclohexanecarbimidic acid | ||
| Canonical SMILES | ClC1=C(C=C(C=C1)NC([C@]2(CCCC[C@]2(C(O)=N)[H])[H])=O)Cl | ||
| 分子式 | C14H16Cl2N2O2 | 分子量 | 315.2 |
| 溶解度 | ≥ 31.5mg/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 | 3.1726 mL | 15.8629 mL | 31.7259 mL |
| 5 mM | 0.6345 mL | 3.1726 mL | 6.3452 mL |
| 10 mM | 0.3173 mL | 1.5863 mL | 3.1726 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。